mAChR1

mAChR1 Related Products (111):

By Type:	Pan (22) Selective (9)
By Effects:	Inhibitors (12) Agonists (31) Antagonists (46) Activators (2) Modulators (16)

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-17360

Tiotropium Bromide	Antagonist	99.91%
Tiotropium bromide (BA-679 BR) is a long-acting anticholinergic bronchodilator. Tiotropium bromide blocks the action of acetylcholine at muscarinic M1, M2, and M3 receptors, prevents bronchoconstriction, and dilates bronchial airways. Tiotropium bromide is applicable to research related to chronic obstructive pulmonary disease and asthma.

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-183144

Vedaclidine	Modulator
Vedaclidine is an orally active muscarinic acetylcholine receptor (mAChR) modulator with mixed receptor activity, which activates muscarinic M2 and M4 receptors and blocks muscarinic M1, M3 and M5 receptors. Vedaclidine exerts its activity through interaction with spinal M4 muscarinic receptors, and does not induce hypothermia or excessive salivation. Vedaclidine can be used in research related to pain, neuropathic pain and inflammatory pain states.

HY-180143

VU6052254	Modulator
VU6052254, a derivative of VU0467319 (HY-173396), is a selective, potent, orally active and brain-penetrant muscarinic M1 acetylcholine receptor (mAChR1) positive allosteric modulator with an EC₅₀ of 59 nM. VU6052254 has no activity on the M2-5 receptor (EC₅₀ > 30 μM). VU6052254 can improve memory recognition ability and reverse the cognitive impairment induced by Scopolamine (HY-N0296) with minimum effective dose both of 1 mg/kg. VU6052254 can be used for the research of neurological disease, such as Alzheimer's disease.

HY-182587

VU0415248	Inhibitor
VU0415248 is a selective muscarinic acetylcholine receptor 1 (M1) inhibitor. VU0415248 inhibits acetylcholine-induced calcium mobilization in cells expressing human and rat M1 muscarinic acetylcholine receptors, with an IC₅₀ of 0.4 and 0.18 μM, respectively. VU0415248 is applicable to the research of Parkinson's disease, movement disorders and fragile X syndrome.

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-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-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-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-17037

Pirenzepine dihydrochloride	Antagonist	99.84%
Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist, with poor penetration of the blood-brain barrier. 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-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-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-15618

MK-7622	Agonist	99.80%
MK-7622 (M1 receptor modulator) is an orally active positive allosteric modulator of muscarinic M1 acetylcholine receptors (mAChRs). MK-7622 enhances ACh-induced calcium flux in CHO cells expressing human M1 receptors (EC₅₀ = 21 nM) and shows robust agonist activity in rat M1-expressing CHO cells, increasing intracellular calcium. MK-7622 reverses Scopolamine (HY-N0296)-induced cognitive deficits in rhesus macaques in an object retrieval detour task. MK-7622 can be used for the study of Alzheimer's disease (AD).

HY-A0082

Diphenidol hydrochloride	Antagonist	99.06%
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-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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