human m4 receptor

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。

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。

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.

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

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

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)

VU6000918 is a positive allosteric modulator that targets the muscarinic acetylcholine receptor subtype M4. It exhibits a half maximal effective concentration (EC50) of 19 nM for the human M4 receptor.

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。

PCS1055 是一种毒蕈碱型M4受体 (muscarinic M4 receptor) 的选择性与竞争性拮抗剂，具有IC50值为18.1 nM 和 Kd值为5.72 nM。此化合物能够抑制放射性配体 [3H]-NMS 与 M4 受体的结合，显示出Ki值为6.5 nM。PCS1055 同时具备AChE抑制活性，对电鳗和人类AChE的IC50分别是22 nM和120 nM。