Agomelatine
Cat. No.:YN321108
CAS No. :138112-76-2
产品名称: | Agomelatine |
CAS No.: | 138112-76-2 |
Chemical Name: | N-[2-(7-methoxy-1-naphthalenyl)ethyl]-acetamide |
Synonyms: | 阿戈美拉汀; S-20098 |
分子量: | 243.30 |
分子式: | C₁₅H₁₇NO₂ |
SMILES: | CC(NCCC1=C2C=C(OC)C=CC2=CC=C1)=O |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | Agomelatine (S-20098) 是一种MT1和MT2受体的特异性激动剂,对 CHO-hMT1,HEK-hMT1,CHO-hMT2,HEK-hMT2 的Ki分别为 0.1,0.06,0.12 和 0.27 nM。Agomelatine 还是一种选择性的5-HT2C受体拮抗剂,在天然 (猪) 和克隆的人 5-HT2C 受体中pKi分别为 6.4 和 6.2。 |
IC50和靶点: | [{name:"5-HT2C Receptor:6.4 (pKi, native porcine)"},{name: "5-HT2C Receptor:6.2 (pKi, human)"},{name: "hMT1:0.1 nM (Ki, CHO Cells)"},{name: "hMT1:0.06 nM (Ki, HEK Cells)"},{name: "hMT2:0.12 nM (Ki, CHO Cells)"},{name: "hMT2:0.27 nM (Ki, HEK Cells)"}] |
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Poissonnier-Durieux, S., Ettaoussi, M., Pérès, B., et al.Synthesis of 3-phenylnaphthalenic derivatives as new selective MT2 melatoninergic ligandsBioorg. Med. Chem.16(18),8339-8348(2008)
Millan, M.J., Gobert, A., Lejeune, F., et al.The novel melatonin agonist agomelatine (S20098) is an antagonist at 5-hydroxytryptamine2C receptors, blockade of which enhances the activity of frontocortical dopaminergic and adrenergic pathwaysJ. Pharmacol. Exp. Ther.306(3),954-964(2003)
Barden, N., Shink, E., Labbé, M., et al.Antidepressant action of agomelatine (S 20098) in a transgenic mouse modelProg. Neuropsychopharmacol. Biol. Psychiatry29(6),908-916(2005)