muscarinic m receptor

SCH 57790 是一种新型且具有选择性的毒蕈碱 M（2） 受体拮抗剂，可释放乙酰胆碱并增强实验动物的认知能力，可用于治疗阿尔茨海默病。

mTOR HDAC-IN-1 (Compound 50) 是一个具有选择性的mTOR 和HDAC 双重抑制剂，对mTOR 和HDAC1的IC50分别为0.49和0.91 nM。 mTOR HDAC-IN-1 可作为抗癌活性分子 （anti-cancer） 进行研究。该化合物的粉末形式不稳定，建议选择其他盐形式产品。

β2AR M-receptor agonist-2 是毒蕈碱拮抗剂和β2 肾上腺素受体激动剂 (MABA)。β2AR M-receptor agonist-2 对 β2 肾上腺素受体的EC50值为 3.7 nM。β2AR M-receptor agonist-2 对人 M3 受体的Ki 值为 0.73 nM。β2AR M-receptor agonist-2 是一种有效的支气管扩张剂，可用于慢性阻塞性肺疾病 (COPD) 的研究。

PF-4348235 HCl (β2AR M-receptor agonist-2 HCl) 是毒蕈碱M3 受体拮抗剂（Ki：0.73 nM）和 β2 肾上腺素受体激动剂 (MABA，EC50：3.7 nM)。PF-4348235 HCl 也是一种支气管扩张剂，可用于研究慢性阻塞性肺疾病 (COPD) 等心血管疾病和呼吸道疾病。

Bencycloquidium Bromide is a muscarinic M3 antagonist. Bencycloquidium bromide inhibits nasal hypersecretion in a rat model of allergic rhinitis. Bencycloquidium Bromide showed high affinity toward the M(3) receptor in Chinese hamster ovary (CHO) cells (M(1) pKi=7.86, M(2) pKi=7.21, M(3) pKi=8.21); pA(2)=8.85, 8.71 and 8.57 in methacholine-induced contraction of trachea, ileum and urinary bladder, 8.19 in methacholine-induced bradycardia of right atrium in vitro, respectively.This compound is unstable in powder form and other related salt forms are recommened.

Peimisine (Ebeiensine) 非竞争性拮抗气管平滑肌 M 受体，抑制 Ach 引起的平滑肌收缩。它兴奋 β 受体和拮抗内钙释放，促进一氧化氮释放，可舒张气管平滑肌，有平喘作用。

(R)-Mequitazine, a muscarinic acetylcholine receptor (M-AChRs) antagonist, is used potentially for the treatment of asthma.

Arecaidine propargyl ester is an agonist of M2muscarinic acetylcholine receptors (mAChRs).1It selectively binds to M2over M1, M3, M4, and M5mAChRs in CHO cells expressing the human receptors (Kis = 0.0871, 1.23, 0.851, 0.977, and 0.933 μM, respectively). Arecaidine propargyl ester induces contractions in isolated guinea pig atrium (pD2= 8.67). It induces apoptosis and the production of reactive oxygen species (ROS) in U87 and U251 glioblastoma cells when used at a concentration of 100 μM.2Arecaidine propargyl ester decreases mean arterial blood pressure in normotensive cats (ED25= 1.9 nmol kg).3It is toxic to house flies (Musca) when administered at a dose of 75 μg fly.4 1.Scapecchi, S., Matucci, R., Bellucci, C., et al.Highly chiral muscarinic ligands: the discovery of (2S,2’R,3’S,5’R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonistJ. Med. Chem.49(6)1925-1931(2006) 2.Di Bari, M., Tombolillo, B., Conte, C., et al.Cytotoxic and genotoxic effects mediated by M2 muscarinic receptor activation in human glioblastoma cellsNeurochem. Int.90261-270(2015) 3.Porsius, A.J., and Van Zwieten, P.A.Central action of some cholinergic drugs (arecaidine esters) and nicotine on blood pressure and heart rate of catsProg. Brain Res.47131-135(1977) 4.Honda, H., Tomizawa, M., and Casida, J.E.Insect muscarinic acetylcholine receptor: Pharmacological and toxicological profiles of antagonists and agonistsJ. Agric. Food Chem.55(6)2276-2281(2007)

Methoctramine is a selective antagonist of M2 muscarinic acetylcholine receptors (IC50 = 6.1 nM in CHO-K1 cell membranes).[1] It is selective for M2 over M1, M3, M4, and M5 receptors (IC50s = 92, 770, 260, and 217 nM, respectively). In vitro, methoctramine inhibits acetylcholine-induced reductions in isolated guinea pig tracheal tube contractions when used at a concentration of 1 μM.[2] In vivo, methoctramine inhibits bradycardia and bronchoconstriction induced by acetylcholinein guinea pigs with ED50 values of 38 and 81 nmol kg, respectively. In a rat model of spinal cord injury, methoctramine suppresses bladder overactivity induced by the non-selective muscarinic acetylcholine receptor agonist oxotremorine M.[3]

NNC-11-1585 is an M(1) and M(2) muscarinic acetylcholine receptor (mAChR) agonist.

β2AR M-receptor agonist-1 (example 131) 为一种结合β2 肾上腺素能受体激动剂功能与毒蕈碱拮抗剂属性的MABA。其对β2 肾上腺素能受体的EC50 值为9.2 nM，对毒蕈碱受体的Ki 值为30.2 nM，展现出强大的MABA效能，EC50值仅为4.0 nM。