Search Result
Results for "
mAChR
" in MedChemExpress (MCE) Product Catalog:
19
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-12426A
-
|
mAChR
|
Neurological Disease
|
mAChR-IN-1 hydrochloride is a potent muscarinic cholinergic receptor (mAChR) antagonist, with an IC50 of 17 nM .
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-
-
- HY-155367
-
|
mAChR
|
Neurological Disease
|
mAChR antagonist 1 (compound 4a) is a mAChR antagonist with Ki values of 255 nM, 121 nM, 158 nM, and 255 nM for M1, M3, M4, and M5 subtype, respectively .
|
-
-
- HY-147028
-
-
-
- HY-101239
-
|
mAChR
|
Neurological Disease
|
Oxotremorine sesquifumarate is a mAChR agonist that mainly activates M2 receptors. Oxotremorine sesquifumarate can be used for neurological research .
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-
-
- HY-119226
-
|
mAChR
|
Neurological Disease
|
VU0152099 is a potent, selective and brain-penetrant mAChR M4 positive allosteric modulator with an EC50 of 0.4 µM for rat M4 receptor. VU0152099 is inactive for other mAChR subtypes or other GPCRs. VU0152099 has no agonist activity but potentiated responses of M4 to acetylcholine .
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-
-
- HY-12439
-
ML380
1 Publications Verification
|
mAChR
|
Neurological Disease
|
ML380 is a potent, subtype-selective, and brain-penetrant positive allosteric modulator (PAM) of M5 mAChR, with EC50s of 190 and 610 nM for human and rat M5, respectively. ML380 exhibits moderate selectivity versus the M1 and M3 mAChR subtypes. ML380 could increase the affinity of ACh for the M5 mAChR .
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-
-
- HY-101839
-
VU0488130
|
mAChR
|
Neurological Disease
|
ML381 (VU0488130) is a highly selective, central nervous system penetrant mAChR M5 orthogonal antagonist (IC50 = 450 nM; Ki = 340 nM). ML381 is unstable in rat plasma and can be mainly used as a molecular probe for in vitro and electrophysiological studies .
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-
-
- HY-12426
-
|
mAChR
|
Neurological Disease
|
mAChR-IN-1 is a potent muscarinic cholinergic receptor (mAChR) antagonist, with an IC50 of 17 nM .
|
-
-
- HY-159177
-
|
mAChR
|
Neurological Disease
|
M4 mAChR Modulator-1 (compound 23i) is a M4 mAChR positive allosteric modulator (PAM). M4 mAChR Modulator-1 exhibits significantly greater cooperativity with ACh in β-arrestin recruitment over G protein activation. M4 mAChR Modulator-1 displays weak PAM effect in G protein-mediated responses, but strong PAM effect in β-arrestin recruitment .
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-
-
- HY-120682
-
|
mAChR
|
Neurological Disease
|
UH-AH 37 is a muscarinic (mAChR) antagonist. UH-AH 37 exhibits a higher potency in inhibiting muscarinic responses in intestinal tissue than cardiac tissue .
|
-
-
- HY-116569
-
-
-
- HY-137388A
-
p-Fluorohexahydrosiladifenidol hydrochloride
|
mAChR
|
Neurological Disease
|
p-F-HHSiD (p-Fluorohexahydrosiladifenidol) hydrochloride is a selective M3 mAChR antagonist. p-F-HHSiD hydrochloride blocks Acetylcholine-mediated vasodilatation in human umbilical vein endothelial cells (HUVECs) .
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-
-
- HY-119333
-
|
mAChR
|
Neurological Disease
|
NNC 11-1607 is a selective M1/M4 muscarinic acetylcholine receptor (mAChR) agonist. NNC 11-1607 inhibits Forskolin (HY-15371)-stimulated cAMP accumulation in Chinese hamster ovary cells expressing the human M2 or M4 mAChR. NNC 11-1607 is promising for research of central nervous system disorders, such as Alzheimer’s disease and schizophrenia .
|
-
-
- HY-B0499A
-
Octylonium bromide; SP63
|
mAChR
|
Neurological Disease
|
Otilonium bromide (OB) is an orally active mAChR inhibitor and smooth muscle relaxant which can interfere with the mobilization of calcium in intestinal smooth muscle, OB can be used for research of irritable bowel syndrome .
|
-
-
- HY-114933
-
|
mAChR
|
Metabolic Disease
|
VU0119498 is a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM), with EC50s of 6.04, 6.38, and 4.08 µM, respectively. VU0119498 has antidiabetic activity .
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-
-
- HY-120576
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VU0405652
|
mAChR
|
Neurological Disease
|
ML169 (VU0405652) is a potent, selective and brain penetrant positive allosteric modulator (PAM) of M1 mAChR, with an EC50 of 1.38 µM. ML169 is a MLPCN probe and can be used for Alzheimer’s disease .
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-
-
- HY-B0499AR
-
|
mAChR
|
Neurological Disease
|
Otilonium (bromide) (Standard) is the analytical standard of Otilonium (bromide). This product is intended for research and analytical applications. Otilonium bromide (OB) is an orally active mAChR inhibitor and smooth muscle relaxant which can interfere with the mobilization of calcium in intestinal smooth muscle, OB can be used for research of irritable bowel syndrome .
|
-
-
- HY-148502
-
|
mAChR
|
Neurological Disease
|
VU6019650 is a potent and selective orthosteric antagonist of M5 mAChR (IC50=36 nM), can be used for opioid use disorder (OUD) relief. VU6019650 can cross blood brain barrier, potentially modulates the mesolimbic dopaminergic reward circuitry. VU6019650 blocks Oxotremorine M iodide (HY-101372A) induced increases of neuronal firing rates of midbrain dopamine neurons in the ventral tegmental area (VTA) .
|
-
-
- HY-124223
-
|
mAChR
|
Neurological Disease
|
AF-DX 384 (methanesulfonate) is a selective antagonist of M2 and M4 muscarinic acetylcholine receptors (Kis=6.03 and 10 nM, respectively) . AF-DX 384 (methanesulfonate) reverses deficits in novel object recognition and passive avoidance in aged rats, as well as in young rats with impairments induced by scopolamine .
|
-
-
- HY-B1205
-
Atropine
Maximum Cited Publications
17 Publications Verification
Tropine tropate; DL-Hyoscyamine
|
mAChR
Endogenous Metabolite
|
Cardiovascular Disease
Neurological Disease
Cancer
|
Atropine (Tropine tropate) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine inhibits ACh-induced relaxations in human pulmonary veins. Atropine can be used for research of anti-myopia and bradycardia .
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-
-
- HY-12100
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GSK573719A
|
mAChR
|
Inflammation/Immunology
Cancer
|
Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.
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-
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- HY-U00079A
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FK-176
|
mAChR
|
Neurological Disease
|
Vamicamide (FK-176) is an orally active competitive mAChR antagonist that inhibits contractions induced by cholinergic nerve stimulation by preventing mAChR agonists from binding to mAChR. Vamicamide exhibits a good anti-bladder spasm effect, with a pA2 value of 6.82 in bladder tissue. Vamicamide can be used in research within the field of neurological diseases .
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-
-
- HY-B0394
-
Tropine tropate sulfate monohydrate; DL-Hyoscyamine sulfate monohydrate
|
mAChR
|
Cardiovascular Disease
Neurological Disease
Cancer
|
Atropine (Tropine tropate) sulfate monohydrate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate monohydrate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate monohydrate can be used for research of anti-myopia and bradycardia .
|
-
-
- HY-B1205B
-
Tropine tropate hydrobromide; DL-Hyoscyamine hydrobromide
|
mAChR
|
Cardiovascular Disease
Neurological Disease
Cancer
|
Atropine (Tropine tropate) hydrobromide is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine hydrobromide inhibits ACh-induced relaxations in human pulmonary veins. Atropine hydrobromide can be used for research of anti-myopia and bradycardia .
|
-
-
- HY-B1205A
-
Tropine tropate sulfate; DL-Hyoscyamine sulfate; Sulfatropinol
|
mAChR
|
Cardiovascular Disease
Neurological Disease
Cancer
|
Atropine (Tropine tropate) sulfate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate can be used for research of anti-myopia and bradycardia .
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-
-
- HY-B2070
-
-
-
- HY-U00119
-
-
-
- HY-B0406
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Carbamyl-β-methylcholine
|
mAChR
|
Neurological Disease
Cancer
|
Bethanechol (Carbamyl-β-methylcholine), a parasympathomimetic agent, is a mAChR agonist that exerts its effects via directly stimulating the mAChR (M1, M2, M3, M4, and M5) of the parasympathetic nervous system .
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- HY-B0406A
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Carbamyl-β-methylcholine chloride
|
mAChR
|
Neurological Disease
Cancer
|
Bethanechol chloride (Carbamyl-β-methylcholine chloride), a parasympathomimetic agent, is a mAChR agonist that exerts its effects via directly stimulating the mAChR (M1, M2, M3, M4, and M5) of the parasympathetic nervous system .
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-
-
- HY-129826
-
|
mAChR
|
Others
|
J-104129 is a selective and orally active muscarinic M3 receptor antagonist (Ki = 4.2 nM). J-104129 is effective in promoting bronchodilation .
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- HY-U00139
-
-
-
- HY-101858
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-
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- HY-B1205R
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Tropine tropate (Standard); DL-Hyoscyamine (Standard)
|
Reference Standards
mAChR
Endogenous Metabolite
|
Cardiovascular Disease
Neurological Disease
|
Atropine (Standard) is the analytical standard of Atropine. This product is intended for research and analytical applications. Atropine (Tropine tropate) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine inhibits ACh-induced relaxations in human pulmonary veins. Atropine can be used for research of anti-myopia and bradycardia .
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-
-
- HY-100916
-
-
-
- HY-B0394R
-
|
mAChR
|
Cardiovascular Disease
Neurological Disease
|
Atropine (sulfate monohydrate) (Standard) is the analytical standard of Atropine (sulfate monohydrate). This product is intended for research and analytical applications. Atropine (Tropine tropate) sulfate monohydrate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate monohydrate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate monohydrate can be used for research of anti-myopia and bradycardia .
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-
-
- HY-B1205AR
-
|
mAChR
|
Cardiovascular Disease
Neurological Disease
|
Atropine (sulfate) (Standard) is the analytical standard of Atropine (sulfate). This product is intended for research and analytical applications. Atropine (Tropine tropate) sulfate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate can be used for research of anti-myopia and bradycardia .
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-
-
- HY-12100S
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GSK573719A-d5
|
Isotope-Labeled Compounds
mAChR
|
Inflammation/Immunology
|
Umeclidinium-d5 (bromide) is the deuterium labeled Umeclidinium bromide. Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.
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-
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- HY-12100S1
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GSK573719A-d10
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mAChR
|
Inflammation/Immunology
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Umeclidinium-d10 (bromide) is the deuterium labeled Umeclidinium bromide. Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.
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-
-
- HY-W309130
-
|
mAChR
|
Neurological Disease
|
(S)-Tolterodine is a muscarinic acetylcholine receptor (mAChR) inhibitor, with an IC50 of 588 nM .
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-
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- HY-12100R
-
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mAChR
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Inflammation/Immunology
Cancer
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Umeclidinium (bromide) (Standard) is the analytical standard of Umeclidinium (bromide). This product is intended for research and analytical applications. Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.
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-
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- HY-B0406AS
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Carbamyl-β-methylcholine-d6 chloride
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Isotope-Labeled Compounds
mAChR
|
Neurological Disease
|
Bethanechol-d6 (chloride) is the deuterium labeled Bethanechol chloride. Bethanechol chloride (Carbamyl-β-methylcholine chloride), a parasympathomimetic agent, is a mAChR agonist that exerts its effects via directly stimulating the mAChR (M1, M2, M3, M4, and M5) of the parasympathetic nervous system .
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- HY-43711
-
|
mAChR
|
Neurological Disease
|
Nor-benzetimide is a major metabolite of Benzetimide. Benzetimide is a mAChR antagonist with anticholinergic activity .
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- HY-14563
-
|
mAChR
|
Neurological Disease
|
VU10010 is a potent, highly selective and allosteric M4 mAChR potentiator with an EC50 of 400 nM. VU10010 binds to an allosteric site on M4 mAChR and increases affinity for acetylcholine and coupling to G proteins. VU10010 increases carbachol-induced depression of transmission at excitatory but not inhibitory synapses in the hippocampus .
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-
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- HY-105771
-
|
mAChR
|
Neurological Disease
|
Parapenzolate bromide, an antispasmodic, is an orally active mAChR antagonist. Parapenzolate bromide is an anticholinergic agent .
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-
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- HY-U00106
-
-
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- HY-N0340
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Hyoscine butylbromide; (-)-Scopolamine butylbromide; Butylscopolamine bromide
|
mAChR
|
Neurological Disease
|
Scopolamine butylbromide is a competitive antagonist of muscarinic acetylcholine receptor (mAChR) with an IC50 of 55.3 ± 4.3 nM.
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-
-
- HY-108234
-
VU 255035
|
mAChR
|
Neurological Disease
|
VU0255035 is a highly selective and competitive M1 mAChR antagonist. VU0255035 blocks M1 mAChR signals to reduce epileptic seizures and regulate neuronal membrane potential. VU0255035 can be used in research related to central nervous system diseases, such as epilepsy, Parkinson's disease, and dystonia .
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-
-
- HY-121404
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(+)-Muscarine
|
mAChR
|
Neurological Disease
|
Muscarine ((+)-Muscarine) is an agonist of prototype mAChR. Muscarine is a toxin that can stimulate the parasympathetic nervous system .
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-
-
- HY-137040A
-
|
mAChR
|
Neurological Disease
|
Tiemonium iodide is a mAChR antagonist with antispasmodic properties. Tiemonium iodide can be used in nervous system research .
|
-
-
- HY-121404A
-
(+)-Muscarine chloride
|
mAChR
|
Neurological Disease
|
Muscarine ((+)-Muscarine) chloride is an agonist of prototype mAChR. Muscarine chloride is a toxin that can stimulate the parasympathetic nervous system .
|
-
- HY-121404B
-
(+)-Muscarine tosylate
|
mAChR
|
Neurological Disease
|
Muscarine ((+)-Muscarine) tosylate is an agonist of prototype mAChR. Muscarine tosylate is a toxin that can stimulate the parasympathetic nervous system .
|
-
- HY-U00105
-
|
mAChR
|
Inflammation/Immunology
|
Oxitropium bromide is an mAChR antagonist used as an anticholinergic bronchodilator agent for the treatment of asthma and chronic obstructive pulmonary disease.
|
-
- HY-16423
-
Org 9487
|
mAChR
|
Neurological Disease
|
Rapacuronium bromide (Org 9487), a non-depolarizing neuromuscular blocker, is an allosteric modulator of muscarinic acetylcholine receptor (mAChR) .
|
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- HY-173031
-
|
mAChR
|
Neurological Disease
|
KTX-005 is the agonist for mAChR that regulates the signaling pathway of the neurotransmitter acetylcholine, and can be used for research of schizophrenia .
|
-
- HY-117284
-
|
mAChR
|
Neurological Disease
|
Eucatropine is a potent muscarinic acetylcholine receptor (mAChR) inhibitor with an IC50 value of 0.583 μM. Eucatropine is an anticholinergic agent .
|
-
- HY-15851
-
-
- HY-116490
-
|
mAChR
|
Cardiovascular Disease
|
Guvacoline hydrobromide, a pyridine alkaloid found in Areca triandra, can act as a weak full agonist of atrial and ileal mAChR .
|
-
- HY-141711
-
|
mAChR
|
Neurological Disease
|
VU6028418 is a potent, highly selective and orally bioavailable M4 mAChR antagonist with an IC50 of 4.1 nM against hM4 .
|
-
- HY-B1719A
-
|
mAChR
|
Inflammation/Immunology
|
Oxyphenonium bromide is an antiacetylcholine compound. Oxyphenonium bromide is an antagonist of mAChR. Oxyphenonium bromide protects against the bronchial obstructive effects .
|
-
- HY-12157
-
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mAChR
|
Others
|
VU 0238429 is positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5), with an EC50 of 1.16 μM.
|
-
- HY-B1789
-
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mAChR
|
Neurological Disease
|
Telenzepine is an antimuscarinic agent with Kis of 0.94 nM (M1 mAChR) and 17.8 nM (M2 mAChR) binding to muscarinic receptors. Telenzepine effectively blocks synaptic transmission promoted by muscarinic or M1 receptor agonists. Thus, Telenzepine can reduce the amplitude of extracellular slow excitatory postsynaptic potentials (EC50=38 nM) and slow inhibitory postsynaptic potentials (EC50=253 nM) .
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-
- HY-169178
-
|
mAChR
|
Neurological Disease
|
VU6016235 is a highly selective, orally available, positive allosteric modulator of the M4 mAChR with in vivo inhibitory potency in animal models of psychosis. .
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- HY-P0102
-
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mAChR
|
Neurological Disease
|
Dipeptide diaminobutyroyl benzylamide diacetate, a Wagerlin-1-mimicking peptide, is a mAChR antagonist. Dipeptide diaminobutyroyl benzylamide diacetate can induce muscle relaxation .
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-
- HY-131574
-
|
mAChR
|
Neurological Disease
|
Heliosupine N-oxide, Heliosupin metabolite, inhibits muscarinic acetylcholine receptor (mAChR) with the IC50 of 350 μM. Heliosupine N-oxide is a pyrrolizidine alkaloid (PA) .
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- HY-17360
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BA679 BR
|
mAChR
|
Neurological Disease
|
Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
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- HY-170032
-
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mAChR
|
Neurological Disease
|
Oxotremorine is an agonist for mAChR, that activates M1 and M3 acetylcholine receptors. Oxotremorine exhibits nicotine-like effects in drug discrimination experiments in macaques .
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-
- HY-W037331
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Bis(4-fluorophenyl)methanol
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mAChR
|
Others
|
4,4-Difluorobenzhydrol is a precursor of a mAChR antagonist, and its derivative 4,4-Difluorobenzhydrol Carbamate can selectively target the M1 subtype .
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-
- HY-160440A
-
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mAChR
|
Neurological Disease
|
VU6021625 is a selective antagonist muscarinic acetylcholine receptors (mAChRs), with the IC50 value of 0.44 nM, 57 nM for human M4 and rat M4, respectively .
|
-
- HY-U00104
-
|
mAChR
|
Endocrinology
|
YM-46303 is an mAChR antagonist which exhibits the highest affinities for M1 and M3 receptors, and selectivity for M3 over M2 receptor.
|
-
- HY-117966
-
|
mAChR
|
Cardiovascular Disease
|
Bibn 140 is a pyridine derivative substituted with a benzene ring, which has high affinity (Ki: 12 nM) and selectivity for M2 mAChR receptors over M1 receptors .
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-
- HY-W739521
-
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mAChR
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Others
|
N-Desethyloxybutynin hydrochloride is an active metabolite of Oxybutynin. N-Desethyloxybutynin hydrochloride binds to mAChRs in isolated? human bladder and human parotid gland with pKi values of 8.2 and 8.7, respectively .
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- HY-B1223
-
|
mAChR
|
Neurological Disease
Cancer
|
Anethole trithione, a sulfur heterocyclic choleretic, is a bile secretion-stimulating agent. Anethole trithione enhances salivary secretion and increases mAChRs, and can be used for dry mouth research .
|
-
- HY-101372A
-
|
mAChR
|
Neurological Disease
|
Oxotremorine M iodide is a potent and non-selective muscarinic acetylcholine receptor (mAChR) agonist. Oxotremorine M iodide potentiates NMDA receptors by muscarinic receptor dependent and independent mechanisms .
|
-
- HY-15502
-
-
- HY-B0394S
-
Tropine tropate-d5; DL-Hyoscyamine-d5
|
mAChR
Autophagy
|
Neurological Disease
|
Atropine-d5 is the deuterium labeled Atropine (sulfate monohydrate). Atropine (Tropine tropate) sulfate monohydrate is a broad-spectrum and competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect .
|
-
- HY-B1188A
-
|
mAChR
|
Neurological Disease
|
Propantheline is an orally active mAChR antagonist. Propantheline can be used in the research of smooth muscle dysfunction, excessive sweating, cramps or spasms of the stomach, intestines or bladder, and involuntary urination .
|
-
- HY-119772
-
ML137
|
Cholinesterase (ChE)
|
Neurological Disease
|
VU0366369 (ML137) is a selective positive allosteric modulator (PAM) for mAChR M1 with an EC50 of 830 nM. VU0366369 can be used in research about central nervous system diseases .
|
-
- HY-100795
-
(±)-Pirmenol; CI-845 free base
|
mAChR
Potassium Channel
|
Cardiovascular Disease
|
Pirmenol is an orally active antiarrhythmic agent. Pirmenol inhibits IK.ACh (IC50: 0.1 μM) by blocking mAchR. Pirmenol can be used in the research of cardiovascular disease, such as atrial fibrillation .
|
-
- HY-B1188
-
|
mAChR
|
Neurological Disease
|
Propantheline bromide is an orally active mAChR antagonist. Propantheline bromide can be used in the research of smooth muscle dysfunction, excessive sweating, cramps or spasms of the stomach, intestines or bladder, and involuntary urination .
|
-
- HY-101694
-
AWD 26-06 free base
|
mAChR
|
Inflammation/Immunology
|
Siltenzepine (AWD 26-06 free base) is an antagonist of mAChR with anti-acid activity, which can be used in peptic ulcers research. Siltenzepine exhibits rapidly but incompletely absorbed characterastic in rats (po) .
|
-
- HY-15851R
-
|
mAChR
|
Cardiovascular Disease
Inflammation/Immunology
|
Revefenacin (Standard) is the analytical standard of Revefenacin. This product is intended for research and analytical applications. Revefenacin (TD-4208; GSK1160724) is a potent mAChR antagonist; has a high affinity on M3 receptor with a Ki of 0.18 nM.
|
-
- HY-100795A
-
(±)-Pirmenol hydrochloride; CI-845
|
mAChR
Potassium Channel
|
Cardiovascular Disease
|
Pirmenol ((±)-Pirmenol) hydrochloride is an orally active antiarrhythmic agent. Pirmenol hydrochloride inhibits IK.ACh (IC50: 0.1 μM) by blocking mAchR. Pirmenol hydrochloride can be used in the research of cardiovascular disease, such as atrial fibrillation .
|
-
- HY-15116
-
|
Prolyl Endopeptidase (PREP)
|
Neurological Disease
|
ONO 1603, a novel prolyl endopeptidase inhibitor investigated as a potential antidementia drug, demonstrated neuroprotective and neurotrophic effects in cerebellar granule cells similar to tetrahydroaminoacridine (THA). At a concentration of 0.03 microM, ONO 1603 promoted neuronal survival, enhanced neurite outgrowth, increased m3-muscarinic acetylcholine receptor (mAChR) mRNA levels, and stimulated mAChR-mediated signaling pathways. These findings suggest that ONO 1603 shares pharmacological similarities with THA, indicating its potential as a therapeutic agent for Alzheimer's disease by enhancing cholinergic neurotransmission and neuronal function .
|
-
- HY-119918
-
|
mAChR
|
Neurological Disease
|
Cycrimine is an orally active muscarinic cholinergic receptor (mAChR) M1 antagonist, reduces the acetylcholine levels in parkinson model. Cycrimine shows antispasmodic activity, can be used in studies of behavioral and mental disorder .
|
-
- HY-17360S
-
BA679 BR-d3
|
Isotope-Labeled Compounds
mAChR
|
Neurological Disease
|
Tiotropium-d3 (bromide) is the deuterium labeled Tiotropium (Bromide). Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
|
-
- HY-B0461
-
|
mAChR
|
Neurological Disease
|
Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors .
|
-
- HY-17360S1
-
BA679 BR-d6
|
Isotope-Labeled Compounds
mAChR
|
Neurological Disease
|
Tiotropium-d6 (bromide) is deuterium labeled Tiotropium (Bromide). Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
|
-
- HY-128783
-
|
mAChR
|
Neurological Disease
|
VU0090157 is a positive allosteric modulator (PAM) of the M1 muscarinic acetylcholine receptor (mAChR). VU0090157 increases the affinity of ACh by binding to the allosteric site. VU0090157 can be used in the study of schizophrenia and Alzheimer's disease .
|
-
- HY-17647R
-
|
DNA/RNA Synthesis
Bacterial
Antibiotic
|
Infection
|
Oxyphenonium (bromide) (Standard) is the analytical standard of Oxyphenonium (bromide). This product is intended for research and analytical applications. Oxyphenonium bromide is an antiacetylcholine compound. Oxyphenonium bromide is an antagonist of mAChR. Oxyphenonium bromide protects against the bronchial obstructive effects .
|
-
- HY-149732
-
|
mAChR
|
Neurological Disease
|
M1/M4 muscarinic agonist 3 (compound 44) is a muscarinic mAChR M1/M4 agonist with EC50s of 31 nM and 9.3 nM, respectively .
|
-
- HY-B0954A
-
|
mAChR
|
Endocrinology
|
Oxyphencyclimine is an orally active muscarinic receptor (mAChR) antagonist. Oxyphencyclimine is effective in reducing ulceration index and increasing pepsin activity in rat gastric ulcer model. Oxyphencyclimine can be used in studies of peptic ulcer disease and gastrointestinal spasm .
|
-
- HY-W318577
-
|
Opioid Receptor
|
Neurological Disease
|
4-Hydroxy-1-(2-phenylethyl)piperidine is a building block that has been used in the synthesis of ligands of the muscarinic acetylcholine receptor (mAChR) or sigma non-opioid intracellular receptor 1 (σ1 receptor).
|
-
- HY-112209
-
|
mAChR
|
Neurological Disease
|
VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (mAChR), potentiating the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey M4 receptor, respectively.
|
-
- HY-B1719AR
-
|
mAChR
|
Inflammation/Immunology
|
Oxyphenonium (bromide) (Standard) is the analytical standard of Oxyphenonium (bromide). This product is intended for research and analytical applications. Oxyphenonium bromide is an antiacetylcholine compound. Oxyphenonium bromide is an antagonist of mAChR. Oxyphenonium bromide protects against the bronchial obstructive effects .
|
-
- HY-12567A
-
(R)-VU0483253
|
Drug Isomer
|
Others
|
(R)-ML375 ((R)-VU0483253) is an enantiomer of ML375 (HY-12567). (R)-ML375 is devoid of M5 mAChR activity (hM5, IC50>30 μM) .
|
-
- HY-B1806A
-
Pathilon chloride
|
mAChR
|
Neurological Disease
Inflammation/Immunology
|
Tridihexethyl (Pathilon) chloride is an orally active anticholinergic agent and mAChR antagonist, shows activities of antimuscarinic and anticholinergic. Tridihexethyl chloride shows pronounced antispasmodic and antisecretory effects on the gastrointestinal tract. Tridihexethyl chloride can be used in studies of peptic ulcer disease and acquired nystagmus .
|
-
- HY-15851S1
-
-
- HY-15851S2
-
-
- HY-15851S3
-
-
- HY-118356
-
|
Neurokinin Receptor
mAChR
|
Neurological Disease
|
WIN 62,577 is a rat-specific, but non-human, NK1 receptor antagonist. WIN 62,577 interacts with M1-M4 mAChRs and is an allosteric enhancer of acetylcholine affinity targeting the M3 receptor.
|
-
- HY-17037
-
LS 519; Pirenzepin dihydrochloride; Gastrozepin dihydrochloride
|
mAChR
|
Metabolic Disease
Cancer
|
Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
|
-
- HY-17360R
-
BA679 BR (Standard)
|
mAChR
|
Neurological Disease
|
Tiotropium (Bromide) (Standard) is the analytical standard of Tiotropium (Bromide). This product is intended for research and analytical applications. Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
|
-
- HY-160440
-
|
mAChR
Drug Isomer
|
Others
|
rel-VU6021625 is the relative configuration of VU6021625 (HY-160440A). VU6021625 is a potent and selective mAChR M4 antagonist with IC50 values of 0.44 nM and 57 nM for human M4, rat M4, respectively .
|
-
- HY-B0549A
-
Rec-7-0040; DW61
|
Phosphodiesterase (PDE)
Calcium Channel
mAChR
|
Neurological Disease
|
Flavoxate hydrochloride is a potent and competitive phosphodiesterase (PDE) inhibitor. Flavoxate hydrochloride is an antispasmodic agent and muscarinic mAChR antagonist. Flavoxate hydrochloride shows moderate calcium antagonistic activity and local anesthetic effect. Flavoxate hydrochloride can be used for the research of overactive bladder (OAB) and lower urinary tract infections .
|
-
- HY-17037A
-
LS 519 free base; Pirenzepin; Gastrozepin
|
mAChR
|
Metabolic Disease
Cancer
|
Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells .
|
-
- HY-B0549
-
Rec-7-0040 free base; DW61 free base
|
Phosphodiesterase (PDE)
Calcium Channel
mAChR
|
Neurological Disease
|
Flavoxate is a potent and competitive phosphodiesterase (PDE) inhibitor. Flavoxate is an antispasmodic agent and muscarinic mAChR antagonist. Flavoxate shows moderate calcium antagonistic activity and local anesthetic effect. Flavoxate can be used for the research of overactive bladder (OAB) and lower urinary tract infections .
|
-
- HY-112076A
-
Methylatropine nitrate; Atropine methyl nitrate
|
mAChR
|
Neurological Disease
|
Atropine methyl bromide, a muscarinic receptor (mAChR) antagonist, is a quaternary ammonium salt of atropine and a mydriatic for dilation of the pupil during ophthalmic examination. It is introduced for relieving pyloric spasm in infants for its highly polar nature. It penetrates less readily into the central nervous system than atropine .
|
-
- HY-112076
-
Methylatropine bromide
|
mAChR
|
Neurological Disease
|
Atropine methyl bromide, a muscarinic receptor (mAChR) antagonist, is a quaternary ammonium salt of atropine and a mydriatic for dilation of the pupil during ophthalmic examination. It is introduced for relieving pyloric spasm in infants for its highly polar nature. It penetrates less readily into the central nervous system than atropine .
|
-
- HY-101679
-
|
mAChR
|
Neurological Disease
|
YM-58790 is a potent antagonist of mAChR. YM-58790 binds M1, M2, M3 with Ki values of 28 nM, 260 nM, and 15 nM. YM-58790 exhibits potent inhibitory activity on bladder pressuer in reflexly-evoked rhythmic contraction in rats .
|
-
- HY-108171A
-
|
mAChR
|
Inflammation/Immunology
|
Hexocyclium methylsulfate is a potent mAChR antagonist with pKi values of 8.9, 7.7, 8.4, 8.8 for M1, M2, M3, and M4 subtype, respectively. Hexocyclium methylsulfate has the potential for the research of duodenal ulcer and irritable bowel syndrome .
|
-
- HY-B1296S1
-
-
- HY-B0461S
-
|
Isotope-Labeled Compounds
mAChR
|
Neurological Disease
|
Trospium-d8 (chloride) is the deuterium labeled Trospium chloride. Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors .
|
-
- HY-159578S
-
|
mAChR
|
Neurological Disease
|
VU6036864 (compound 45) is an orally active, selective mAChR M5 antagonist with IC50=20 nM for human M5. VU6036864 is >500-fold selective for human M1-4, with BBB characteristic and high oral bioavailability (%F>100%) .
|
-
- HY-107651
-
|
mAChR
|
Metabolic Disease
|
VU 0365114 is a selective mAChR M5 positive allosteric modulator, with an EC50 of 2.7 μM, and >30 μM for M1, M2, M3 and M4 receptors. VU 0365114 increases insulin secretion stimulated by ACh in human β-cells .
|
-
- HY-B1188R
-
|
mAChR
|
Neurological Disease
|
Propantheline (bromide) (Standard) is the analytical standard of Propantheline (bromide). This product is intended for research and analytical applications. Propantheline bromide is an orally active mAChR antagonist. Propantheline bromide can be used in the research of smooth muscle dysfunction, excessive sweating, cramps or spasms of the stomach, intestines or bladder, and involuntary urination .
|
-
- HY-122743
-
Iperoxo
1 Publications Verification
|
mAChR
|
Neurological Disease
|
Iperoxo is a potent superagonist of muscarinic acetylcholine receptor (mAChR) that activates M1, M2 and M3 receptors with pEC50 of 9.87, 10.1 and 9.78. Iperoxo can be used for direct probing activation-related conformational transitions of muscarinic receptors when labeled with tritium .
|
-
- HY-149731
-
|
mAChR
|
Neurological Disease
|
M1/M2/M4 muscarinic agonist 2 (compound 43) is a muscarinic mAChR M1/M2/M4 agonist with EC50s of 30 nM, 200 nM and 6.2 nM, respectively .
|
-
- HY-B0461R
-
|
mAChR
|
Neurological Disease
|
Trospium (chloride) (Standard) is the analytical standard of Trospium (chloride). This product is intended for research and analytical applications. Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors .
|
-
- HY-157956
-
|
mAChR
|
Neurological Disease
|
LASSBio-873 is an orally active muscarinic cholinergic receptor (mAChR) agonist that crosses the blood-brain barrier. LASSBio-873 has potent analgesic effects on acute and inflammatory pain. The analgesic effect of LASSBio-873 can be inhibited by intrathecal injection of the M2 receptor antagonist methoctramine .
|
-
- HY-12158
-
|
mAChR
|
Neurological Disease
|
VU0238441 is a pan muscarinic acetylcholine receptor (mAChR) positive allosteric modulator (PAM) with EC50s of 3.2 μM, 2.8 μM, 2.2 μM, 2.1 μM, >10 μM for M1, M2, M3, M5 and M4, respectively .
|
-
- HY-101679A
-
|
mAChR
|
Neurological Disease
|
YM-58790 free base is a potent antagonist of mAChR. YM-58790 free base binds M1, M2, M3 with Ki values of 28 nM, 260 nM, and 15 nM. YM-58790 free base exhibits potent inhibitory activity on bladder pressuer in reflexly-evoked rhythmic contraction in rats .
|
-
- HY-12567
-
VU0483253
|
mAChR
|
Neurological Disease
|
ML375 (VU0483253) is a potent, highly selective, brain-penetrant and orally active M5 mAChR negative allosteric modulator (NAM) with IC50s of 300 nM and 790 nM for human and rat M5, respectively. ML375 is inactive at human and rat M1-M4 .
|
-
- HY-A0030
-
|
mAChR
|
Neurological Disease
Metabolic Disease
Cancer
|
Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB) .
|
-
- HY-149733
-
|
mAChR
|
Neurological Disease
|
M1/M2/M4 muscarinic agonist 3 (compound 45) is a muscarinic mAChR M1/M2/M4 agonist with EC50s of 3.2 nM, 32 nM and 1.7 nM, respectively .
|
-
- HY-70053
-
|
mAChR
|
Neurological Disease
Metabolic Disease
|
Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine is used for the overactive bladder (OAB) .
|
-
- HY-B0549AR
-
|
Phosphodiesterase (PDE)
Calcium Channel
mAChR
|
Neurological Disease
|
Flavoxate (hydrochloride) (Standard) is the analytical standard of Flavoxate (hydrochloride). This product is intended for research and analytical applications. Flavoxate hydrochloride is a potent and competitive phosphodiesterase (PDE) inhibitor. Flavoxate hydrochloride is an antispasmodic agent and muscarinic mAChR antagonist. Flavoxate hydrochloride shows moderate calcium antagonistic activity and local anesthetic effect. Flavoxate hydrochloride can be used for the research of overactive bladder (OAB) and lower urinary tract infections .
|
-
- HY-B0781
-
|
Histamine Receptor
mAChR
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors .
|
-
- HY-B1343
-
|
Cholinesterase (ChE)
|
Neurological Disease
|
Pridinol mesylate is an orally active, blood-brain permeable, muscarinic acetylcholine receptor (mAChR)-directed muscle relaxant. Pridinol mesylate reduces the conduction of impulses to spinal motor neurons and exerts muscle relaxant activity. Pridinol mesylate inhibits skeletal muscle contractures in diseases of both central and peripheral origin and can be used in research in the field of musculoskeletal diseases .
|
-
- HY-17037R
-
|
mAChR
|
Metabolic Disease
Cancer
|
Pirenzepine (dihydrochloride) (Standard) is the analytical standard of Pirenzepine (dihydrochloride). This product is intended for research and analytical applications. Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
|
-
- HY-B1343A
-
|
Cholinesterase (ChE)
|
Neurological Disease
|
Pridinol is an orally active, blood-brain permeable, muscarinic acetylcholine receptor (mAChR)-directed muscle relaxant. Pridinol reduces the conduction of impulses to spinal motor neurons and exerts muscle relaxant activity. Pridinol inhibits skeletal muscle contractures in diseases of both central and peripheral origin and can be used in research in the field of musculoskeletal diseases .
|
-
- HY-70053A
-
|
mAChR
|
Neurological Disease
Metabolic Disease
Cancer
|
Fesoterodine L-mandelate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine L-mandelate is used for the overactive bladder (OAB) .
|
-
- HY-155819
-
|
mAChR
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
M3/PDE4 modulator-1 (compound 10f) is a bifunctional molecule that is an M3 mAChR antagonist and a PDE4 inhibitor. M3/PDE4 modulator-1 (10-1000 nM/kg; iv) reduces cysteine eosinophil influx in the OVA rat model .
|
-
- HY-16489A
-
|
mAChR
Calcium Channel
|
Neurological Disease
|
Terodiline hydrochloride is an M1-selective muscarinic receptor (mAChR) antagonist with Kbs of 15, 160, 280, and 198 nM in rabbit vas deferens (M1), atria (M2), bladder (M3) and ileal muscle (M3), respectively. Terodiline hydrochloride also is a Ca 2+ blocker. Terodiline hydrochloride acts as a treatment for urinary frequency and urge incontinence .
|
-
- HY-13340
-
VU152100
|
mAChR
|
Neurological Disease
|
VU0152100 (VU152100) is a highly selective mAChR positive allosteric modulator (permeable to the blood-brain barrier). VU0152100 reverses Amphetamine-induced hypermotility in rats and increased levels of extracellular dopamine in nucleus accumbens and caudate-putamen. VU0152100 has good research potential in psychosis and cognitive impairment associated with mental disorders such as schizophrenia .
|
-
- HY-P1376A
-
|
mAChR
Adrenergic Receptor
|
Endocrinology
|
G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis .
|
-
- HY-76570A
-
(Rac)-Desfesoterodine hydrochloride; (Rac)-PNU-200577 hydrochloride
|
mAChR
|
Neurological Disease
|
(Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine) hydrochloride, an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine hydrochloride can be used for overactive bladder research .
|
-
- HY-76569
-
PNU-200577; 5-Hydroxymethyl Tolterodine
|
mAChR
|
Neurological Disease
Cancer
|
Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively . Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053) . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .
|
-
- HY-76570
-
(Rac)-Desfesoterodine; (Rac)-PNU-200577
|
mAChR
|
Neurological Disease
|
(Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research .
|
-
- HY-A0030S
-
|
mAChR
|
Metabolic Disease
|
Fesoterodine-d7 (fumarate) is the deuterium labeled Fesoterodine fumarate . Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB) .
|
-
- HY-B0781S1
-
|
Isotope-Labeled Compounds
mAChR
Adrenergic Receptor
Histamine Receptor
|
Neurological Disease
Endocrinology
|
Promethazine-d3 (hydrochloride) is deuterium labeled Promethazine (hydrochloride). Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors .
|
-
- HY-112076R
-
|
mAChR
|
Neurological Disease
|
Atropine methyl (bromide) (Standard) is the analytical standard of Atropine methyl (bromide). This product is intended for research and analytical applications. Atropine methyl bromide, a muscarinic receptor (mAChR) antagonist, is a quaternary ammonium salt of atropine and a mydriatic for dilation of the pupil during ophthalmic examination. It is introduced for relieving pyloric spasm in infants for its highly polar nature. It penetrates less readily into the central nervous system than atropine .
|
-
- HY-A0030R
-
|
mAChR
|
Neurological Disease
Metabolic Disease
Cancer
|
Fesoterodine (fumarate) (Standard) is the analytical standard of Fesoterodine (fumarate). This product is intended for research and analytical applications. Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB) .
|
-
- HY-17037S1
-
LS 519-d8 dihydrochloride; Pirenzepin-d8 dihydrochloride; Gastrozepin-d8 dihydrochloride
|
Isotope-Labeled Compounds
mAChR
|
Cancer
|
Pirenzepine-d8 (LS 519-d8; Pirenzepin-d8) dihydrochloride is a deuterium labeled Pirenzepine (dihydrochloride) (HY-17037). Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
|
-
- HY-B0781R
-
|
Reference Standards
Histamine Receptor
mAChR
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
Promethazine (hydrochloride) (Standard) is the analytical standard of Promethazine (hydrochloride). This product is intended for research and analytical applications. Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors .
|
-
- HY-B1343AS
-
|
Cholinesterase (ChE)
Isotope-Labeled Compounds
|
Neurological Disease
|
Pridinol-d5 is deuterium labeled Pridinol (HY-B1343A) . Pridinol is an orally active, blood-brain permeable, muscarinic acetylcholine receptor (mAChR)-directed muscle relaxant. Pridinol reduces the conduction of impulses to spinal motor neurons and exerts muscle relaxant activity. Pridinol inhibits skeletal muscle contractures in diseases of both central and peripheral origin and can be used in research in the field of musculoskeletal diseases .
|
-
- HY-107655
-
ABET
|
mAChR
|
Cardiovascular Disease
|
Arecaidine but-2-ynyl ester tosylate (ABET) is a selective mAChR M2 agonist that dose-dependently decreases mean arterial pressure and heart rate in rats. Arecaidine but-2-ynyl ester tosylate can be used for cardiovascular disease research . Arecaidine but-2-ynyl ester (tosylate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-76569R
-
|
mAChR
|
Neurological Disease
|
Desfesoterodine (Standard) is the analytical standard of Desfesoterodine. This product is intended for research and analytical applications. Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively . Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053) . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .
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- HY-B1343R
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Reference Standards
Cholinesterase (ChE)
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Neurological Disease
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Pridinol mesylate (Standard) is the analytical standard of Pridinol mesylate (HY-B1343). This product is intended for research and analytical applications. Pridinol mesylate is an orally active, blood-brain permeable, muscarinic acetylcholine receptor (mAChR)-directed muscle relaxant. Pridinol mesylate reduces the conduction of impulses to spinal motor neurons and exerts muscle relaxant activity. Pridinol mesylate inhibits skeletal muscle contractures in diseases of both central and peripheral origin and can be used in research in the field of musculoskeletal diseases .
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- HY-76569S1
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PNU-200577-d14; 5-Hydroxymethyl Tolterodine-d14
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mAChR
Isotope-Labeled Compounds
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Neurological Disease
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(R)-Hydroxytolterodine-d14 is deuterated labeled Desfesoterodine (HY-76569). Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively . Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053) . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .
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- HY-76570S1
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Isotope-Labeled Compounds
mAChR
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Neurological Disease
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5-Hydroxymethyl Tolterodine-d14 (formate) is deuterium labeled (Rac)-5-Hydroxymethyl Tolterodine. (Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research .
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- HY-76570S
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(Rac)-Desfesoterodine-d14; (Rac)-PNU-200577-d14
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Isotope-Labeled Compounds
mAChR
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Neurological Disease
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(Rac)-5-Hydroxymethyl Tolterodine-d14 is the deuterium labeled (Rac)-5-Hydroxymethyl Tolterodine. (Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research .
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- HY-151801
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mAChR
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Others
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DIBA-Cy5 is a fluorescent DIBA antagonist made up be DIBA-alkyne binding Cyanine5 fluorophores (Cy5) and polyethylene glycol (PEG) biomolecules. DIBA-Cy5 can serve as a fluorescent ligand, suitable for probe attachment through click chemistry. DIBA-Cy5 exerts a high binding affinity to type-2 mAChR (M2R) with the Kd value of 1.80 nM, can directly stain M2R receptors in the sinoatrial node of a mouse heart .
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- HY-14562
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mAChR
Amyloid-β
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Neurological Disease
Inflammation/Immunology
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TBPB (tert-butyl peroxybenzoate) is a highly selective, blood-brain-permeable M1 mAChR allosteric agonist (EC50=289 nM) with anti-schizophrenia and anti-inflammatory activities. TBPB can enhance the sensitivity of M1 receptors to acetylcholine, activate downstream signaling pathways, and inhibit the release of pro-inflammatory cytokines (TNF-α, IL-6). TBPB can regulate the processing of amyloid and can be used in the study of neurodegenerative diseases (such as Alzheimer's disease) and inflammation-related diseases (such as sepsis) .
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- HY-B0267A
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mAChR
Potassium Channel
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Neurological Disease
Cancer
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Oxybutynin chloride is an oral active and competitive mAChR antagonist with Kis of 14.3 and 5.55 nM for specific [ 3H]NMS binding in the mouse bladder and cerebral cortex, respectively. Oxybutynin chloride inhibits vascular Kv channels in a manner independent of anticholinergic effect, with an IC50 value of 11.51 μM. Oxybutynin chloride reduces muscle spasm in the bladder and urinary tract, can be used in study of overactive bladder syndrome (OAB) . Oxybutynin (chloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-P5846
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MT3
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mAChR
Adrenergic Receptor
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Neurological Disease
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Muscarinic toxin 3 (MT3) is a potent and non-competitive mAChR and adrenoceptors antagonist with pIC50s of 6.71, 8.79, 8.86, 7.57, 8.13, 8.49, <6.5, 7.29 against M1, M4, α1A, α1B, α1D,α2A,α2B and α2C receptors, respectively. Muscarinic toxin 3 displays prominent adrenoceptor activity .
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- HY-107111
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mAChR
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Neurological Disease
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GSK1034702 is an orally active and allosteric agonist of M1 mAChR (pEC50=8.1) that can cross the blood-brain barrier. GSK1034702 activates the Gq/11 protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 can be used for the study of the mechanisms of cognitive impairment diseases such as Alzheimer's disease, and has certain peripheral M receptor activation-related side effects (such as gastrointestinal reactions) .
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- HY-B0267AR
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mAChR
Potassium Channel
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Neurological Disease
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Oxybutynin (chloride) (Standard) is the analytical standard of Oxybutynin (chloride). This product is intended for research and analytical applications. Oxybutynin chloride is an oral active and competitive mAChR antagonist with Kis of 14.3 and 5.55 nM for specific [ 3H]NMS binding in the mouse bladder and cerebral cortex, respectively. Oxybutynin chloride inhibits vascular Kv channels in a manner independent of anticholinergic effect, with an IC50 value of 11.51 μM. Oxybutynin chloride reduces muscle spasm in the bladder and urinary tract, can be used in study of overactive bladder syndrome (OAB) . Oxybutynin (chloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-107111A
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Cholinesterase (ChE)
mAChR
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Neurological Disease
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GSK1034702 hydrochloride is an orally active and allosteric agonist of M1 mAChR (pEC50=8.1) that can cross the blood-brain barrier. GSK1034702 hydrochloride activates the Gq/11 protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 hydrochloride can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 hydrochloride can be used for the study of the mechanisms of cognitive impairment diseases such as Alzheimer's disease, and has certain peripheral M receptor activation-related side effects (such as gastrointestinal reactions) .
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HY-L062
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2,170 compounds
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Neurotransmitter (NT) receptors, also known as neuroreceptors, are a broadly diverse group of membrane proteins that bind neurotransmitters for neuronal signaling. There are two major types of neurotransmitter receptors: ionotropic and metabotropic. Ionotropic receptors are ligand-gated ion channels, meaning that the receptor protein includes both a neurotransmitter binding site and an ion channel. The binding of a neurotransmitter molecule (the ligand) to the binding site induces a conformational change in the receptor structure, which opens, or gates, the ion channel. The term “metabotropic receptors” is typically used to refer to transmembrane G-protein-coupled receptors. Metabotropic receptors trigger second messenger-mediated effects within cells after neurotransmitter binding.
In some neurological diseases, the neurotransmitter receptor itself appears to be the target of the disease process. Many neuroactive drugs act by modifying neurotransmitter receptors. A better understanding of neurotransmitter receptor changes in disease may lead to improvements in therapy.
MCE designs a unique collection of 2,170 compounds targeting a variety of neurotransmitter receptors. MCE Neurotransmitter Receptor Compound Library is a useful tool for neurological diseases drug discovery.
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Cat. No. |
Product Name |
Type |
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- HY-151801
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Fluorescent Dyes/Probes
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DIBA-Cy5 is a fluorescent DIBA antagonist made up be DIBA-alkyne binding Cyanine5 fluorophores (Cy5) and polyethylene glycol (PEG) biomolecules. DIBA-Cy5 can serve as a fluorescent ligand, suitable for probe attachment through click chemistry. DIBA-Cy5 exerts a high binding affinity to type-2 mAChR (M2R) with the Kd value of 1.80 nM, can directly stain M2R receptors in the sinoatrial node of a mouse heart .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P0102
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mAChR
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Neurological Disease
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Dipeptide diaminobutyroyl benzylamide diacetate, a Wagerlin-1-mimicking peptide, is a mAChR antagonist. Dipeptide diaminobutyroyl benzylamide diacetate can induce muscle relaxation .
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- HY-P1376A
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mAChR
Adrenergic Receptor
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Endocrinology
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G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis .
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- HY-P5846
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MT3
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mAChR
Adrenergic Receptor
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Neurological Disease
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Muscarinic toxin 3 (MT3) is a potent and non-competitive mAChR and adrenoceptors antagonist with pIC50s of 6.71, 8.79, 8.86, 7.57, 8.13, 8.49, <6.5, 7.29 against M1, M4, α1A, α1B, α1D,α2A,α2B and α2C receptors, respectively. Muscarinic toxin 3 displays prominent adrenoceptor activity .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
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- HY-12100S1
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Umeclidinium-d10 (bromide) is the deuterium labeled Umeclidinium bromide. Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.
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- HY-B0394S
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Atropine-d5 is the deuterium labeled Atropine (sulfate monohydrate). Atropine (Tropine tropate) sulfate monohydrate is a broad-spectrum and competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect .
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- HY-17360S
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Tiotropium-d3 (bromide) is the deuterium labeled Tiotropium (Bromide). Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
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- HY-12100S
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Umeclidinium-d5 (bromide) is the deuterium labeled Umeclidinium bromide. Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.
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- HY-B0406AS
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Bethanechol-d6 (chloride) is the deuterium labeled Bethanechol chloride. Bethanechol chloride (Carbamyl-β-methylcholine chloride), a parasympathomimetic agent, is a mAChR agonist that exerts its effects via directly stimulating the mAChR (M1, M2, M3, M4, and M5) of the parasympathetic nervous system .
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- HY-17360S1
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Tiotropium-d6 (bromide) is deuterium labeled Tiotropium (Bromide). Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
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- HY-15851S1
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Revefenacin-d9 (TD-4208-d9) is deuterium labeled Revefenacin. Revefenacin (TD-4208; GSK1160724) is a potent mAChR antagonist; has a high affinity on M3 receptor with a Ki of 0.18 nM.
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- HY-15851S2
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Revefenacin-d3 (TD-4208-d3) is deuterium labeled Revefenacin. Revefenacin (TD-4208; GSK1160724) is a potent mAChR antagonist; has a high affinity on M3 receptor with a Ki of 0.18 nM.
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- HY-15851S3
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Revefenacin-d4 (TD-4208-d4) is deuterium labeled Revefenacin. Revefenacin (TD-4208; GSK1160724) is a potent mAChR antagonist; has a high affinity on M3 receptor with a Ki of 0.18 nM.
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- HY-B1296S1
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Promethazine-d4 is a deuterated-labeled promethazine (HY-B0781). Promethazine is an orally active H1 receptor and mAChR antagonist with antihistamine (H1), sedative, antiemetic, anticholinergic, and anti-motion sickness properties .
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- HY-B0461S
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Trospium-d8 (chloride) is the deuterium labeled Trospium chloride. Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors .
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- HY-159578S
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VU6036864 (compound 45) is an orally active, selective mAChR M5 antagonist with IC50=20 nM for human M5. VU6036864 is >500-fold selective for human M1-4, with BBB characteristic and high oral bioavailability (%F>100%) .
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- HY-A0030S
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Fesoterodine-d7 (fumarate) is the deuterium labeled Fesoterodine fumarate . Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB) .
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- HY-B0781S1
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Promethazine-d3 (hydrochloride) is deuterium labeled Promethazine (hydrochloride). Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors .
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- HY-17037S1
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Pirenzepine-d8 (LS 519-d8; Pirenzepin-d8) dihydrochloride is a deuterium labeled Pirenzepine (dihydrochloride) (HY-17037). Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
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- HY-B1343AS
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Pridinol-d5 is deuterium labeled Pridinol (HY-B1343A) . Pridinol is an orally active, blood-brain permeable, muscarinic acetylcholine receptor (mAChR)-directed muscle relaxant. Pridinol reduces the conduction of impulses to spinal motor neurons and exerts muscle relaxant activity. Pridinol inhibits skeletal muscle contractures in diseases of both central and peripheral origin and can be used in research in the field of musculoskeletal diseases .
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- HY-76569S1
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(R)-Hydroxytolterodine-d14 is deuterated labeled Desfesoterodine (HY-76569). Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively . Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053) . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .
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- HY-76570S1
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5-Hydroxymethyl Tolterodine-d14 (formate) is deuterium labeled (Rac)-5-Hydroxymethyl Tolterodine. (Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research .
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- HY-76570S
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(Rac)-5-Hydroxymethyl Tolterodine-d14 is the deuterium labeled (Rac)-5-Hydroxymethyl Tolterodine. (Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research .
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Cat. No. |
Product Name |
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Classification |
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- HY-159578S
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Azide
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VU6036864 (compound 45) is an orally active, selective mAChR M5 antagonist with IC50=20 nM for human M5. VU6036864 is >500-fold selective for human M1-4, with BBB characteristic and high oral bioavailability (%F>100%) .
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