muscarinic m4 receptor

PCS1055 dihydrochloride is an effective, selective, and competitive muscarinic M4 receptor antagonist (IC50: 18.1 nM and a Kd: 5.72 nM). PCS1055 dihydrochloride is also a potent AChE inhibitor (IC50 s: 22 nM and 120 nM for electric eel and human AChE, res

RO1138452 (CAY10441) 是一种选择性和可口服的前列环素受体拮抗剂，pKi 为8.3。它拮抗卡前列环素诱导的人神经母细胞瘤腺苷酸环化酶的激活，以剂量依赖性方式阻断环 AMP 积累，具有镇痛活性。

Clozapine N-oxide 是 Clozapine 的主要代谢产物，具有血脑屏障渗透性。Clozapine N-oxide 是一种 DREADDs 激动剂，可激活 DREADD 受体 hM3Dq 和 hM4Di。Clozapine N-oxide 也是一种多巴胺拮抗剂和选择性毒蕈碱 M4 受体激动剂。

Tropicamide (Ro 1-7683) 是一种选择性的 M4毒蕈碱乙酰胆碱受体拮抗剂，作为滴眼剂使用时，会产生短效瞳孔扩张和睫状肌麻痹。

Fesoterodine fumarate (Toviaz) 是可口服的，非亚型选择性的竞争性毒蕈碱受体拮抗剂，用于膀胱过度活动症，对 M1、M2、M3、M4 和 M5 受体的pKi 值分别为 8.0、7.7、7.4、7.3 和 7.5。

DREADD agonist 21 是一种人毒蕈碱乙酰胆碱 M3 受体激动剂，EC50为 1.7 nM。

VU0467154 是 M4 毒蕈碱的乙酰胆碱受体的正向调节剂，能够增强小鼠、人和食蟹猴 M4 受体对乙酰胆碱的反应，pEC50值分别为 7.75、6.2 和 6。

VU10010 (VU 10010) 是一种高度选择性的M4mAChR 变构增强剂，EC50为 400 nM。它与 M4mAChR 的变构位点结合，增强与 G 蛋白偶联，增加对乙酰胆碱的亲和力，还会增加卡巴胆碱引起的兴奋性传导抑制。

VU0152099 是选择性和可透过血脑屏障的 mAChR M4正变构调节剂，可增强 M4 对乙酰胆碱的反应，对大鼠 M4 受体的 EC50为 0.4 µM。

VU0238441是一种泛毒蕈碱型乙酰胆碱受体阳性变构调节剂，对 M1、M2、M3、M5 和 M4 的EC50分别为 3.2、2.8、2.2、2.1 和大于 10 μM。

VU6005806 is a potent positive allosteric modulator (PAM) of muscarinic acetylcholine receptor subtype 4 (M4) (EC50s: 94 nM, 28 nM, 87 nM, and 68 nM for human, rat, dog, and cyno M4, respectively), and used in the study of neuropsychiatric disorders.

Thiochrome is a selective enhancer of M4 muscarinic receptor of acetylcholine (ACh) affinity.

VU0152100 是一种选择性 M4 mAChR 变构增强剂，EC50为 380 ± 93 nM。

VU0467485 is a potent and selective muscarinic acetylcholine receptor 4 positive allosteric modulator. VU0467485 potentiates the activity of ACh at M4 (EC50s: 26.6 nM and 78.8 nM at the rat and human M4 receptors, respectively). VU0467485 displays selecti

Direclidine 作为一种毒蕈碱型 M4 受体 (muscarinic M4 receptor) 正变构调节剂。

VU6016235为口服三环M4毒蕈碱乙酰胆碱受体正变构调节剂，具有高度选择性和独特的结构特征。

Clozapine (HF 1854) dihydrochloride 是用于研究精神疾病的化合物。Clozapine 对多种神经受体展现出高度亲和力，是一种对多巴胺受体的有效拮抗剂，Ki值为 75 nM，并抑制毒蕈碱M1受体和血清素5HT2A受体，Ki值分别为 9.5 nM 和 4 nM。此外，Clozapine 也是毒蕈碱M4受体的选择性激动剂，EC50为11 nM。

AF-DX 384 free base 是一种具有选择性和高效性的 M2 毒蕈碱乙酰胆碱受体 ( M2 mAChR) 和 M4 毒蕈碱乙酰胆碱受体 ( M4 mAChR) 拮抗剂 ，可用于研究神经分裂和帕金森等神经神经系统疾病。

M4 muscarinic receptor antagonist

(S)-(+)-Dimethindene maleate 是一种可口服且具有选择性毒蕈碱 M2 受体和组胺 H1 受体拮抗剂，抑制毒蕈碱 M1，M3 和 M4 受体。

Atropine Oxide is a derivative of Atropine. Atropine is a competitive antagonist of the muscarinic acetylcholine receptor types M1, M2, M3, M4, and M5. Atropine is a medication to treat certain types of nerve agents and pesticide poisonings as well as som

Aclidinium bromide (LAS-W 330) 是长效可吸入型的毒蕈碱拮抗剂，有用于慢性阻塞性肺病 (COPD) 的研究潜力。

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)

Imidafenacin metabolite M4 is a metabolite of the muscarinic acetylcholine receptor antagonist imidafenacin.1It is formed from imidafenacin by the cytochrome P450 (CYP) isoform CYP3A4. 1.Kanayama, N., Kanari, C., Masuda, Y., et al.Drug-drug interactions in the metabolism of imidafenacin: Role of the human cytochrome P450 enzymes and UDP-glucuronic acid transferases, and potential of imidafenacin to inhibit human cytochrome P450 enzymesXenobiotica37(2)139-154(2007)