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-B0461
    Trospium chloride
    		Antagonist 99.93%
    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.
    Trospium chloride
  • HY-A0033
    Darifenacin
    		Antagonist 99.81%
    Darifenacin (UK-88525) is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin inhibits tumor growth in colorectal cancer cells and has anti-tumor effects.
    Darifenacin
  • HY-B0394
    Atropine sulfate monohydrate
    		Antagonist 99.68%
    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.
    Atropine sulfate monohydrate
  • HY-W010892
    Scopolamine hydrobromide trihydrate
    		Antagonist 99.89%
    Scopolamine (Hyoscine) hydrobromide trihydrate is a high-affinity muscarinic antagonist that can cross the blood-brain barrier. Scopolamine hydrobromide trihydrate competitively antagonizes 5-HT3 receptors with an IC50 of 2.09 μM. Scopolamine hydrobromide trihydrate can induce cognitive and memory deficits in animals. Scopolamine hydrobromide trihydrate can be used in the research of preventing postoperative nausea and vomiting, motion sickness, nervous system diseases, etc.
    Scopolamine hydrobromide trihydrate
  • HY-A0030
    Fesoterodine fumarate
    		Antagonist 99.52%
    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).
    Fesoterodine fumarate
  • HY-B1006
    Pilocarpine nitrate
    		Agonist 99.83%
    Pilocarpine nitrate is a potent M3-type muscarinic acetylcholine receptor (M3 muscarinic receptor) agonist.
    Pilocarpine nitrate
  • HY-100234A
    DREADD agonist 21 dihydrochloride
    		Agonist 98.94%
    DREADD agonist 21 dihydrochloride is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist (EC50=1.7 nM).
    DREADD agonist 21 dihydrochloride
  • HY-A0082
    Diphenidol hydrochloride
    		Antagonist 99.95%
    Diphenidol hydrochloride (Difenidol hydrochloride) is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol hydrochloride is also a potent non-specific blocker of voltage-gated ion channels (Na+, K+, and Ca2+) in neuronal cells. Diphenidol hydrochloride can be used in the study of antivertigo and antinausea.
    Diphenidol hydrochloride
  • HY-108234
    VU 0255035
    		Antagonist 99.76%
    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.
    VU 0255035
  • HY-107922
    Ethopropazine hydrochloride
    		Antagonist 99.66%
    Ethopropazine (Isothazine) hydrochloride is a potent and selective BChE inhibitor, a poor AChE inhibitor and a non-selective mAChR and NMDA antagonist. Ethopropazine hydrochloride has anticholinergic, antihistamine, antiadrenergic actions and properties. Ethopropazine hydrochloride alleviates thermal hyperalgesia in a dose dependent manner. Ethopropazine hydrochloride can be used for the research of Parkinson’s disease.
    Ethopropazine hydrochloride
  • HY-N0471
    L-Hyoscyamine
    		Antagonist 99.96%
    L-Hyoscyamine (Daturine), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine is a levo-isomer to Atropine (HY-B1205).
    L-Hyoscyamine
  • HY-70020B
    Cevimeline hydrochloride
    		Agonist 98.74%
    Cevimeline hydrochloride (AF102B hydrochloride) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline hydrochloride can cross the blood-brain barrier (BBB).
    Cevimeline hydrochloride
  • HY-120023
    VU0453595
    		Agonist 99.90%
    VU0453595 is a highly selective, systemically active M1 positive allosteric modulator (PAM, EC50=2140 nM) for the research of schizophrenia.
    VU0453595
  • HY-B0241
    Ipratropium bromide
    		Antagonist 99.92%
    Ipratropium bromide (Sch 1000) 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 relaxes smooth muscle, can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma.
    Ipratropium bromide
  • HY-122190
    TAK-071
    		Modulator 99.44%
    TAK-071 is a novel, potent and highly selective muscarinic acetylcholine receptor 1 (M1R) positive allosteric modulator. EC50 of TAK-071 M1R agonist activities is 520 nM.
    TAK-071
  • HY-76772
    Cevimeline hydrochloride hemihydrate
    		Agonist 99.52%
    Cevimeline hydrochloride hemihydrate (SNI-2011) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride hemihydrate stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline hydrochloride hemihydrate can cross the blood-brain barrier (BBB).
    Cevimeline hydrochloride hemihydrate
  • HY-106432A
    Sabcomeline hydrochloride
    		Agonist 99.86%
    Sabcomeline (SB-202026) hydrochloride is a potent and functionally selective muscarinic M1 receptor partial agonist that improve cognition. Sabcomeline hydrochloride can be used for Alzheimer's disease research.
    Sabcomeline hydrochloride
  • HY-76569
    Desfesoterodine
    		Antagonist 99.66%
    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.
    Desfesoterodine
  • HY-B0549A
    Flavoxate hydrochloride
    		Antagonist 99.70%
    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.
    Flavoxate hydrochloride
  • HY-112209
    VU0467154
    		Agonist 99.24%
    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.
    VU0467154
Cat. No. Product Name / Synonyms Application Reactivity
mAChR Isoform Comparison

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