mAChR1

mAChR1 Related Products (94):

By Type:	Pan (16) Selective (6)
By Effects:	Inhibitors (9) Agonists (25) Antagonists (42) Activators (2) Modulators (12)

Cat. No.	Product Name	Effect	Purity

HY-14539

Clozapine	Modulator	99.84%
Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a K_i of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with K_is of 9.5 nM and 4 nM, respectively. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC₅₀=11 nM).

HY-105182

Xanomeline	Agonist	99.80%
Xanomeline, as an effective and selective muscarinic type 1 and type 4 (M1/M4) receptor agonist, increases neuronal excitability. Xanomeline can be used for the research of neurological disorders, such as schizophrenia.

HY-122743

Iperoxo	Agonist	99.48%
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-107647

(S)-(+)-Dimethindene maleate	Antagonist	99.80%
(S)-(+)-Dimethindene maleate, an enantiomer, is a potent M₂-selective muscarinic receptor antagonist (pA₂ = 7.86/7.74; pK_i = 7.78). (S)-(+)-Dimethindene maleate shows lower affinities for the muscarinic M₁ (pA₂ = 6.83/6.36; pK_i = 7.08), the M₃ (pA₂ = 6.92/6.96; pK_i = 6.70) and the M₄ receptors (pK_i = 7.00), respectively. (S)-(+)-Dimethindene maleate also is a histamine H₁ receptor antagonist (pA₂ = 7.48).

HY-B0406A

Bethanechol chloride	Agonist	99.56%
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.

HY-173396

VU0467319	Modulator	98.53%
VU0467319 (Compound VU319) is a highly selective and blood-brain-permeable, orally active M1 positive allosteric modulator (PAM) (EC₅₀: 492 nM). VU0467319 is selective (EC₅₀ > 30 μM) versus M2-5 for both human and rat. VU0467319 improves cognitive impairment in Alzheimer's disease (AD) through central M1 muscarinic receptors. VU0467319 does not induce cholinergic adverse reactions and has potential in AD research.

HY-118363

Lu AE51090	Agonist
Lu AE51090 is selective muscarinic M1 receptor agonist with blood-brain barrier penetration. Lu AE51090 activates human M1 receptor with EC₅₀ of 61 nM, while showing no significant agonism at M2-M5 receptors. Lu AE51090 exerts procognitive effects in mice. Lu AE51090 can be used for the study of Alzheimer’s disease (AD) and cognitive impairment associated with schizophrenia (CIAS).

HY-177498

M1 mAChR modulator-1	Modulator
M1 mAChR modulator-1 (Example 66) is a muscarinic M1 receptor (mAChR1) positive allosteric modulator. M1 mAChR modulator-1 effectively promotes gastrointestinal motility and defecation in mouse models with low central permeability. M1 mAChR modulator-1 can be used for constipation research.

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).

HY-A0030

Fesoterodine fumarate	Antagonist	99.52%
Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pK_i 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-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.

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.

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.

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.

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.

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.

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).

HY-17037

Pirenzepine dihydrochloride	Antagonist	99.84%
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-76570

(Rac)-5-Hydroxymethyl Tolterodine	Antagonist	99.05%
(Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (K_i 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-32067

Aceclidine	Modulator	99.23%
Aceclidine (Quinuclidin-3-yl acetate) is a modulator of M3 muscarinic acetylcholine receptor and a M1 receptor agonist (EC₅₀: 40 μM). Aceclidine is a cycloplegic agent, a surfactant, a tonicity adjustor and optionally a viscosity enhancer and an antioxidant. Aceclidine has the potential for the research of disorders such as refractive errors of the eye, xerostomia, Sjogren's syndrome, glaucoma, conjunctivitis, lacrimal gland disease, and esotropia.

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