mAChR 选择性抑制剂 | 激动剂 | 拮抗剂 | 调节剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S5258 Revefenacin

Revefenacin (TD-4208, GSK-1160724) is a potent, lung-selective, long-acting muscarinic antagonist that may be for the treatment of respiratory disease.

Selective
S4031 Aclidinium Bromide

Aclidinium Bromide与人源毒蕈碱受体AChR M1, M2, M3, M4和M5结合,Ki值分别为0.1 nM, 0.14 nM, 0.14 nM, 0.21 nM和0.16 nM。

Selective M5 mAChR, Ki: 0.16 nM; M4 mAChR, Ki: 0.21 nM; M1 mAChR, Ki: 0.1 nM; M2 mAChR, Ki: 0.14 nM; M3 mAChR, Ki: 0.14 nM
S9790 JHU37160

JHU37160 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.9 nM and 3.6 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 18.5 nM and 0.2 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.

Selective hM4Di, EC50: 0.2 nM; hM3Dq, EC50: 18.5 nM; hM3Dq, Ki: 1.9 nM; hM4Di, Ki: 3.6 nM
S5385 Imidafenacin

Imidafenacin (KRP-197, ONO-8025) is a urinary antispasmodic of the anticholinergic class. It is a novel antimuscarinic agent with safety and efficacy, has been clinically used for the treatment of overactive bladder. Imidafenacin(KRP-197; ONO-8025) is a potent and selective inhibitor of M3 receptors with Kb of 0.317 nM; less potent for M2 receptors(IC50=4.13 nM). IC50 value: 0.3 nM(M3).

Selective M2 receptor, IC50: 4.13 nM; M3 receptor, Kd: 0.317 nM; M3 receptor, IC50: 0.3 nM
S3913 Pimethixene maleate

Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.

Selective Muscarinic M2, pKi: 9.38; Muscarinic M1, pKi: 8.61
S9789 JHU37152

JHU37152 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.8 nM and 8.7 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 5 nM and 0.5 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.

Selective hM4Di, EC50: 0.5 nM; hM4Di, Ki: 8.7 nM; hM3Dq, EC50: 5 nM; hM3Dq, Ki: 1.8 nM
S2659 5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM)

5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM)是一种新的蕈毒碱受体拮抗剂,Kb为0.84 nM.

Selective mAChR, Kb: 0.84 nM
S3144 Darifenacin HBr

Darifenacin HBr是一种选择性的M3 muscarinic(M3蕈毒碱)受体拮抗剂,pKi为8.9。

Selective M3 mAChR, pKi: 8.9
S0032 Batefenterol 

Batefenterol is a novel muscarinic receptor antagonist and β2-adrenoceptor agonist. Batefenterol displays high affinity for hM2, hM3 muscarinic and hβ2-adrenoceptor with Ki of 1.4 nM, 1.3 nM and 3.7 nM, respectively.

Selective hM3 muscarinic receptor, Ki: 1.3 nM; hM2 muscarinic receptor, Ki: 1.4 nM
S5921 Cyclopentolate Hydrochloride

Cyclopentolate is an antagonist of muscarinic acetylcholine receptors with Ki values of 1.62, 27.5, and 2.63 nM for M1, M2, and M3 receptors, respectively.

Selective M1 receptor, Ki: 1.62 nM; M2 receptor, Ki: 27.5 nM; M3 receptor, Ki: 2.63 nM
S5777 Ipratropium bromide monohydrate

Ipratropium bromide (Atrovent, Sch 1000) monohydrate is an antagonist of muscarinic acetylcholine receptors (mAChR) with IC50 of 2.9 nM, 2.0 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively.

Selective M3 receptor, IC50: 1.7 nM; M2 receptor, IC50: 2.0 nM; M1 receptor, IC50: 2.9 nM
S0457 DREADD agonist 21

DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist with EC50 of 1.7 nM.

Selective hM3Dq, EC50: 1.7 nM
S2130 Atropine sulfate monohydrate

Atropine sulfate monohydrate是一种竞争性毒蕈碱型乙酰胆碱受体拮抗剂,IC50为2.5 nM。

Selective mAChR, IC50: 2.5 nM
S1913 Tropicamide

Tropicamide是一种抗胆碱,毒蕈碱受体M4亚型的选择性拮抗剂,IC50为8.0 nM。

Selective M4 mAChR, IC50: 8 nM
S2508 Scopolamine (LSM-4015) HBr

Scopolamine HBr是一种竞争性的毒蕈碱型乙酰胆碱受体拮抗剂,IC50为55.3 ¡À 4.3 nM。

Selective mAChR, IC50: 55.3 nM
S4024 Homatropine Methylbromide

Homatropine Methylbromide是一种毒蕈碱受体AChR拮抗剂,抑制WKY-E和SHR-E , IC50分别为162.5 nM和170.3 nM。

Selective mAChR (SHR-E), IC50: 170.3 nM; mAChR (WKY-E), IC50: 162.5 nM
S4025 Homatropine Bromide

Homatropine Bromide是一种毒蕈碱受体AChR拮抗剂,抑制WKY-E和SHR-E , IC50分别为162.5 nM和170.3 nM。

Selective mAChR (WKY-E), IC50: 162.5 nM; mAChR (SHR-E), IC50: 170.3 nM
S6795 VU0357017 Hydrochloride

VU0357017 hydrochloride (CID-25010775) is a potent, highly selective and CNS-penetrant agonist of M1 which is a subtype of muscarinic acetylcholine receptors (mAChRs). VU0357017 hydrochloride appears to act at an allosteric site to activate the receptor with EC50 of 477 nM and Ki of 9.91 μM.

Selective M1 mAChR, EC50: 477 nM; M1 mAChR, Ki: 9.91 μM
S2646 VU0238429

VU0238429 (M5 PAM) is the first positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5/M5) with EC50 of 1.16 μM at M5 and both > 30 μM at M1 and M3. VU0238429 shows no potentiator activity at M2 or M4.

Selective M3 mAChR, : ; M1 mAChR, : ; M5 mAChR, IC50: 1.16 μM
S0782 VU0238441

VU0238441 is a potent agonist of human Muscarinic acetylcholine receptor M5 with EC50 of 2.1 μM.

Selective mAChR M4, IC50: >10 μM; mAChR M1, IC50: 3.2 μM; mAChR M2, IC50: 2.8 μM; mAChR M3, IC50: 2.2 μM; mAChR M5, IC50: 2.1 μM
S0783 VU0119498

VU0119498 is an agonist of M1 muscarinic receptor with EC50 of 3.1 μM. VU0119498 is a pan mAChR M3, M5 positive allosteric modulator (PAM) and a neuroprotective agent.

Selective mAChR M1, IC50: 6.1 μM; mAChR M5, IC50: 4.1 μM; mAChR M3, IC50: 6.4 μM
S4027 Flavoxate HCl

Flavoxate HCl是一种毒蕈碱受体AChR拮抗剂, IC50为12.2 μM.

Selective mAChR, IC50: 12.2 μM
S4713 Atropine

Atropine (Atropen, Atnaa, Tropine tropate, DL-Hyoscyamine) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect.

Selective
S2614 Arecoline HBr

Arecoline是一种毒蕈碱型乙酰胆碱受体激动剂。

Selective
S3048 Solifenacin succinate

Solifenacin succinate是一种抗毒蕈碱类泌尿解痉药。

Selective
S5873 Scopolamine HBr trihydrate

Scopolamine HBr is a competitive muscarinic acetylcholine receptor antagonist with an IC50 of 55.3 nM.

Selective
S2455 Bethanechol chloride

Bethanechol chloride是一种选择性毒蕈碱受体激动剂,对烟碱受体没有任何效果。

Selective
S4143 Pentoxyverine Citrate

Pentoxyverine Citrate 是antitussive(止咳药),通常用于治疗咳嗽相关的疾病,如感冒。

Selective
S1929 Irsogladine

Irsogladine是一种抗胃溃疡剂,通过M1 muscarininc乙酰胆碱受体结合,有利于细胞间隙连接通讯。

Selective
S4231 Pilocarpine HCl

Pilocarpine HCl 是非选择性毒蕈碱型乙酰胆碱受体激动剂,用于产生癫痫的实验模型。

Selective
S3117 Oxybutynin hydrochloride

Oxybutynin chloride是一种抗胆碱药,用于缓解尿和膀胱负担。

Selective
S1978 Methscopolamine

Methscopolamine是一种毒蕈碱型乙酰胆碱受体抑制剂。

Selective
S3047 Otilonium Bromide

Otilonium Bromide是一种抗毒蕈碱药物.

Selective
S3735 Umeclidinium bromide

Umeclidinium bromide is a long-acting muscarinic antagonist approved for the maintenance treatment of chronic obstructive pulmonary disease (COPD).

Selective
S1683 Ipratropium Bromide

Ipratropium bromide是毒蕈碱拮抗剂,支气管扩张剂,是AtropineN的异丙基盐。

Selective
S4292 Diphenidol HCl

Diphenidol HCl是一种有效的muscarinic M2 and M3 receptor拮抗剂,pKb分别为6.72和7.02,用于呕吐和晕眩的治疗。

Selective
S4034 Diphemanil Methylsulfate

Diphemanil Methylsulfate是一种季铵抗胆碱能药剂,可以结合毒蕈碱型乙酰胆碱受体(mAchR)。

Selective