2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. mAChR

mAChR

Muscarinic acetylcholine receptor

mAChR

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mAChRs (muscarinic acetylcholine receptors) are acetylcholine receptors that form G protein-receptor complexes in the cell membranes of certainneurons and other cells. They play several roles, including acting as the main end-receptor stimulated by acetylcholine released from postganglionic fibersin the parasympathetic nervous system. mAChRs are named as such because they are more sensitive to muscarine than to nicotine. Their counterparts are nicotinic acetylcholine receptors (nAChRs), receptor ion channels that are also important in the autonomic nervous system. Many drugs and other substances (for example pilocarpineand scopolamine) manipulate these two distinct receptors by acting as selective agonists or antagonists. Acetylcholine (ACh) is a neurotransmitter found extensively in the brain and the autonomic ganglia.

mAChR Isoform Specific Products:

mAChR Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-12439
    ML380
    		Agonist 99.91%
    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.
    ML380
  • HY-12157
    VU 0238429
    		Agonist 99.96%
    VU 0238429 is positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5), with an EC50 of 1.16 μM.
    VU 0238429
  • HY-122203
    PCS1055 dihydrochloride
    		Antagonist 98.88%
    PCS1055 dihydrochloride is a potent, selective and competitive muscarinic M4 receptor antagonist with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 dihydrochloride exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 dihydrochloride is also a potent AChE inhibitor with IC50 s of 22 nM and 120 nM for electric eel and human AChE, respectively.
    PCS1055 dihydrochloride
  • HY-B0547A
    Homatropine Bromide
    		Antagonist 99.99%
    Homatropine Bromide is an orally active muscarinic acetylcholine receptor antagonist and can be used as an anticholinergic agent.
    Homatropine Bromide
  • HY-B1621A
    Cyclopentolate hydrochloride
    		Antagonist 99.54%
    Cyclopentolate (DL-Cyclopentolate) hydrochloride is an Atropine-like muscarinic receptors antagonist with a pKB value of 7.8 (on the circular ciliary muscle). Cyclopentolate hydrochloride is an anti-muscarinic agent commonly used in the ophthalmologic practice.
    Cyclopentolate hydrochloride
  • HY-107646
    PD 102807
    		Antagonist 98.52%
    PD 102807 is a M4 muscarinic receptor antagonist with an IC50 of 90.7 nM. PD 102807 inhibits M1, M2, M3, M5 muscarinic receptor with IC50s of 6558.7, 3440.7, 950.0, and 7411.7 nM, respectively. Antidyskinetic effect.
    PD 102807
  • HY-B0327
    Irsogladine
    		Inhibitor 99.97%
    Irsogladine is a PDE4 inhibitor and muscarinic acetylcholine receptor binder.
    Irsogladine
  • HY-N0340
    Scopolamine butylbromide
    		Antagonist 99.97%
    Scopolamine butylbromide is a competitive antagonist of muscarinic acetylcholine receptor (mAChR) with an IC50 of 55.
    Scopolamine butylbromide
  • HY-15851
    Revefenacin
    		Antagonist 99.23%
    Revefenacin (TD-4208; GSK1160724) is a potent mAChR antagonist; has a high affinity on M3 receptor with a Ki of 0.18 nM.
    Revefenacin
  • HY-B1205S
    (Rac)-Atropine-d3
    		99.07%
    (Rac)-Atropine-d3 is the deuterium labeled (Rac)-Atropine[1].
    (Rac)-Atropine-d<sub>3</sub>
  • HY-128855
    Talsaclidine
    		Agonist 98.75%
    Talsaclidine is a muscarinic agonist with preferential neuron-stimulating properties. Talsaclidine is a full agonist at the M1 subtype, and as a partial agonist at the M2 and M3 subtypes. Talsaclidine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Talsaclidine
  • HY-P1376A
    G-Protein antagonist peptide TFA
    		Inhibitor
    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.
    G-Protein antagonist peptide TFA
  • HY-114933
    VU0119498
    		Modulator 99.52%
    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.
    VU0119498
  • HY-134004
    Pentoxyverine
    		Antagonist 98.91%
    Pentoxyverine (Carbetapentane) is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membran σ1, respectively. Pentoxyverine is a muscarinic antagonist. Pentoxyverine is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance.
    Pentoxyverine
  • HY-116408A
    Propiverine hydrochloride
    		Inhibitor 99.89%
    Propiverine hydrochloride is a bladder spasmolytic with calcium antagonistic and anticholinergic properties. Propiverine hydrochloride can be used for the research of overactive blaqdder and urinary incontinence.
    Propiverine hydrochloride
  • HY-12100
    Umeclidinium bromide
    		Antagonist 99.72%
    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.
    Umeclidinium bromide
  • HY-105296
    Blarcamesine
    		Modulator 99.51%
    Blarcamesine is an orally bioavailable Sigma-1 receptor agonist and muscarinic receptor modulator, with anticonvulsant, anti-amnesic, neuroprotective and antidepressant properties. Blarcamesine ameliorates neurologic impairments in a mouse model of Rett syndrome.
    Blarcamesine
  • HY-B1332
    Ipratropium bromide hydrate
    		Antagonist 99.90%
    Ipratropium bromide (Sch 1000) hydrate is a muscarinic receptor antagonist, with IC50s of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide hydrate relaxes smooth muscle, can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma.
    Ipratropium bromide hydrate
  • HY-B2070
    Methylbenactyzium Bromide
    		Inhibitor 99.53%
    Methylbenactyzium Bromide is a muscarinic acetylcholine receptor (mAChR) inhibitor.
    Methylbenactyzium Bromide
  • HY-12980
    Batefenterol
    		Antagonist 99.72%
    Batefenterol (GSK961081;TD-5959) is a novel muscarinic receptor antagonist and β2-adrenoceptor agonist; displays high affinity for hM2, hM3 muscarinic and hβ2-adrenoceptor with Ki values of 1.4, 1.3 and 3.7 nM, respectively.
    Batefenterol
Cat. No. Product Name / Synonyms Application Reactivity
mAChR Isoform Comparison

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