Search Result
Results for "
cholinergic antagonist
" in MedChemExpress (MCE) Product Catalog:
6
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-12426A
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mAChR
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Neurological Disease
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mAChR-IN-1 hydrochloride is a potent muscarinic cholinergic receptor (mAChR) antagonist, with an IC50 of 17 nM .
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- HY-B0461
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mAChR
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Neurological Disease
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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-B0461R
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mAChR
Reference Standards
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Neurological Disease
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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 .
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- HY-B0303A
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- HY-U00139
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- HY-B1585
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Parpanil
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iGluR
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Neurological Disease
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Parpanil is an anticholinergic agent with NMDA receptor antagonist activity. Parpanil can be used to inhibit diseases related to cholinergic neurotransmission. Parpanil exerts its pharmacological effects by blocking cholinergic effects .
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- HY-167699
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mAChR
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Others
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Cyclodrine is a cholinergic receptor antagonist that exhibits biological activity by influencing both muscarinic and nicotinic receptors.
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- HY-12426
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mAChR
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Neurological Disease
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mAChR-IN-1 is a potent muscarinic cholinergic receptor (mAChR) antagonist, with an IC50 of 17 nM .
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- HY-N15736
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mAChR
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Neurological Disease
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Petiline is a steroidal alkaloid found in Petilium raddeanum, acting as a selective antagonist of M cholinergic receptors. Petiline exerts anticholinergic effects (e.g., reducing vagal influence on the heart) by competitively blocking M cholinergic receptors, and also has central excitatory, cardiotonic, and spasmolytic activities. Petiline is promising for research of cholinergic system-related diseases (e.g., arrhythmia, intestinal spasm) .
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- HY-B0461S
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Isotope-Labeled Compounds
mAChR
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Neurological Disease
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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-B0303
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- HY-19489S1
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- HY-P3162
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- HY-138973A
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iGluR
nAChR
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Neurological Disease
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Neramexane mesylate is an α9α10 cholinergic nicotinic receptors and N-methyl-D-aspartate receptors(NMDA) antagonist. Neramexane mesylate can improve moderate to severe tinnitus, and also shows neuroprotective effects .
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- HY-119918
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mAChR
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Neurological Disease
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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 .
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- HY-W040055A
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L-erythro-Neopterin
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mAChR
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Neurological Disease
Metabolic Disease
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L-(-)-Neopterin (L-erythro-Neopterin) is a cholinergic receptor that acts as a competitive antagonist, countering the inhibitory effects of pteridine diuretics on the growth of Crithidia fasciculata. L-(-)-Neopterin can be used in research related to the nervous system and purine metabolism .
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- HY-P3162A
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- HY-B0303AS1
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- HY-B0303AS
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- HY-B0303AR
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- HY-135740
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- HY-B0303R
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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-157956
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mAChR
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Neurological Disease
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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 .
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- HY-100979
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HDMPPA
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mAChR
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Others
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W-84 (dibromide) is a potent allosteric modulator of M2-cholinoceptors, which retards [ 3H]N-methylscopolamine dissociation. W-84 dibromide can stabilize cholinergic antagonist-receptor complexes. W-84 (dibromide) is a non-competitive muscarinic acetylcholine receptors antagonist with allosteric effects. W-84 (dibromide) protects over additively against an organophosphate-intoxication when applied in combination with atropine .
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- HY-B1690AR
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Reference Standards
Antibiotic
Bacterial
Histamine Receptor
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Infection
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Thioridazine (Standard) is the analytical standard of Thioridazine. This product is intended for research and analytical applications. Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs) .
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- HY-B1690
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Antibiotic
Bacterial
Histamine Receptor
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Infection
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Methdilazine is an orally active antibiotic (histamine antagonist). Methdilazine can inhibit various mycobacterium with MIC values at 5-15 μg/mL in vitro and in vivo, which can be used for the research of infectious diseases .
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- HY-B1690A
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Antibiotic
Bacterial
Histamine Receptor
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Infection
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Methdilazine hydrochloride is an orally active antibiotic (histamine antagonist). Methdilazine hydrochloride can inhibit various mycobacterium with MIC values at 5-15 μg/mL in vitro and in vivo, which can be used for the research of infectious diseases .
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- HY-U00079A
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FK-176
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mAChR
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Neurological Disease
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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-B1339
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Dicycloverine hydrochloride
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mAChR
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Neurological Disease
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Dicyclomine hydrochloride is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine hydrochloride shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .
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- HY-B1339A
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Dicycloverine
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mAChR
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Neurological Disease
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Dicyclomine (Dicycloverine) is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine (Dicycloverine) shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .
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- HY-172884
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Cholinesterase (ChE)
iGluR
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Neurological Disease
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MDAR IN-1 (Compound 5m) is a brain-penetrant inhibitor of acetylcholinesterase (AChE) and antagonist of the GluN1/GluN2B subtype of NMDAR receptor. MDAR IN-1 effectively inhibits AChE activity, enhances cholinergic neurotransmission, and blocks NMDAR, reducing excitatory neurotoxicity. MDAR IN-1 is promising for research of Alzheimer's disease .
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- HY-B1339AS
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Dicycloverine-d4
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mAChR
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Neurological Disease
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Dicyclomine-d4 is the deuterium labeled Dicyclomine . Dicyclomine (Dicycloverine) is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine (Dicycloverine) shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .
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- HY-B1339R
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Dicycloverine hydrochloride (Standard)
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Reference Standards
mAChR
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Neurological Disease
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Dicyclomine (hydrochloride) (Standard) is the analytical standard of Dicyclomine (hydrochloride). This product is intended for research and analytical applications. Dicyclomine hydrochloride is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine hydrochloride shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .
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- HY-110155
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Neurotensin Receptor
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Neurological Disease
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LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 dihydrochloride is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. LM11A-31 dihydrochloride reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression .
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- HY-117088
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LM11A-31
Maximum Cited Publications
7 Publications Verification
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Neurokinin Receptor
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Neurological Disease
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LM11A-31, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. LM11A-31 reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression .
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- HY-B1339S
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Dicycloverine-d4 hydrochloride
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Isotope-Labeled Compounds
mAChR
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Neurological Disease
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Dicyclomine-d4 hydrochloride (Dicycloverine-d4 hydrochloride) is the deuterium labeled Dicyclomine hydrochloride (HY-B1339). Dicyclomine hydrochloride is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine hydrochloride shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .
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- HY-118056
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Cannabinoid Receptor
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ABD459 is a CB1 receptor antagonist with significant effects on regulating food intake and sleep-wake cycles. ABD459 completely displaces CB1 agonist CP99540 (Ki = 8.6 nM) and antagonizes CP55940-induced GTPγS binding (KB = 7.7 nM). ABD459 may specifically modulate endogenous cannabinoid release through cholinergic activity and plays a role in attention and arousal regulation. ABD459 is suitable for research in neurological disorders .
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- HY-P11313
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Rat chromogranin A367–387
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nAChR
Akt
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Cardiovascular Disease
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Catestatin (rat) (Rat chromogranin A367–387) is a potent, reversible, noncompetitive, and noncooperative nicotinic cholinergic antagonist derived from chromogranin A(A367-387). Catestatin (rat) inhibits norepinephrine release in rat PC12 pheochromocytoma cells (IC50 = 1.2 μM), and blocks desensitization of norepinephrine release (IC50 = 0.62 μM). Catestatin (rat) exerts antiadrenergic effects through the endothelial PI3K-AKT-eNOS pathway in rat papillary muscles and isolated cardiomyocytes. Catestatin (rat) maintains mitochondrial membrane potential in I/R cardiomyocytes and increases phosphorylation of AKT at S473, GSK3β at S9, PLB at T17, and eNOS at S1179. Catestatin (rat) reverses desensitization of 22Na + uptake. Catestatin (rat) can be used for the study of nicotinic cholinergic receptor regulation and catecholamine release control mechanisms .
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- HY-B1693
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Methotrimeprazine
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5-HT Receptor
Dopamine Receptor
Histamine Receptor
Autophagy
Enterovirus
Calcium Channel
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Infection
Neurological Disease
Inflammation/Immunology
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Levomepromazine (Methotrimeprazine) is an orally active antipsychotic compound and Ca 2+ release inducer. Levomepromazine inhibits SERCA pump and induces an increase in cytoplasmic Ca 2+ levels. Levomepromazine has antagonistic effects on a variety of neurotransmitter receptors, including dopamine, cholinergic, serotonin, and histamine receptors. Levomepromazine can induce adaptive ER stress and autophagy. In addition, Levomepromazine has antiviral, anti-inflammatory, neuroprotective and analgesic, sedative and anti-injurious activities. Levomepromazine can be used in the study psychiatric disorders and relieving nausea and vomiting .
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- HY-B1693R
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Methotrimeprazine (Standard)
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Reference Standards
5-HT Receptor
Dopamine Receptor
Autophagy
Histamine Receptor
Enterovirus
Calcium Channel
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Infection
Neurological Disease
Inflammation/Immunology
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Levomepromazine (Standard) is the analytical standard of Levomepromazine. This product is intended for research and analytical applications. Levomepromazine (Methotrimeprazine) is an orally active antipsychotic compound and Ca 2+ release inducer. Levomepromazine inhibits SERCA pump and induces an increase in cytoplasmic Ca 2+ levels. Levomepromazine has antagonistic effects on a variety of neurotransmitter receptors, including dopamine, cholinergic, serotonin, and histamine receptors. Levomepromazine can induce adaptive ER stress and autophagy. In addition, Levomepromazine has antiviral, anti-inflammatory, neuroprotective and analgesic, sedative and anti-injurious activities. Levomepromazine can be used in the study psychiatric disorders and relieving nausea and vomiting .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P3162A
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- HY-P1376A
-
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mAChR
Adrenergic Receptor
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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 .
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- HY-P3162
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- HY-P11313
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Rat chromogranin A367–387
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nAChR
Akt
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Cardiovascular Disease
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Catestatin (rat) (Rat chromogranin A367–387) is a potent, reversible, noncompetitive, and noncooperative nicotinic cholinergic antagonist derived from chromogranin A(A367-387). Catestatin (rat) inhibits norepinephrine release in rat PC12 pheochromocytoma cells (IC50 = 1.2 μM), and blocks desensitization of norepinephrine release (IC50 = 0.62 μM). Catestatin (rat) exerts antiadrenergic effects through the endothelial PI3K-AKT-eNOS pathway in rat papillary muscles and isolated cardiomyocytes. Catestatin (rat) maintains mitochondrial membrane potential in I/R cardiomyocytes and increases phosphorylation of AKT at S473, GSK3β at S9, PLB at T17, and eNOS at S1179. Catestatin (rat) reverses desensitization of 22Na + uptake. Catestatin (rat) can be used for the study of nicotinic cholinergic receptor regulation and catecholamine release control mechanisms .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
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- HY-B0303AS1
-
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Diphenhydramine-d5 (hydrochloride) is the deuterium labeled Diphenhydramine hydrochloride. Diphenhydramine hydrochloride is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB) .
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- HY-B0303AS
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Diphenhydramine-d6 (hydrochloride) is the deuterium labeled Diphenhydramine hydrochloride. Diphenhydramine hydrochloride is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB) .
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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-19489S1
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(Rac)-Levomepromazine-d3 (hydrochloride) is a labelled racemic Methotrimeprazine, which is a phenothiazine which has antagonist actions at multiple neurotransmitter receptor sites, including dopaminergic, cholinergic, serotonin and histamine receptors .
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- HY-B1339AS
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Dicyclomine-d4 is the deuterium labeled Dicyclomine . Dicyclomine (Dicycloverine) is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine (Dicycloverine) shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .
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- HY-B1339S
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Dicyclomine-d4 hydrochloride (Dicycloverine-d4 hydrochloride) is the deuterium labeled Dicyclomine hydrochloride (HY-B1339). Dicyclomine hydrochloride is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine hydrochloride shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .
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