盐酸阿戈美拉汀 T60523

Product Introduction
Bioactivity


英文名: Agomelatine hydrochloride

描述: Agomelatine hydrochloride (S-20098 hydrochloride) (S-20098 hydrochloride) 是特异性的MT1和MT2受体激动剂，对 CHO-hMT1的Ki 值为0.1 nM，对HEK-hMT1的Ki 值为0.06 nM，对CHO-hMT2的Ki 值为0.12 nM，对HEK-hMT2 的Ki 值为0.27 nM。Agomelatine hydrochloride 是选择性的5-羟色胺2C(5-HT2C)受体拮抗剂，对天然 (猪) 和克隆的人 5-HT2C 受体的pKi 值分别为 6.4 和 6.2。

体外活性: Agomelatine (S 20098) acts as a full agonist of MT1 and MT2 receptors with EC50s of 1.6±0.4, 0.10±0.04 nM for CHO hMT1 CHO-hMT2 (hΜΤ1 and hΜΤ2 receptors expressed in CHO or HEK cell membranes)[1]. Agomelatine (S20098) also interacts with h5-HT2B receptors (6.6), whereas it shows low affinity at native (rat)/cloned, human 5-HT2A (<5.0/5.3) and 5-HT1A (<5.0/5.2) receptors, and negligible (<5.0) affinity for other 5-HT receptors[2].

体内活性: Agomelatine (25, 50, or 75 mg/kg; i.p.) has antioxidant activity in Strychnine (75 mg/kg, i.p.) or Pilocarpine (400 mg/kg, i.p.) induced seizure models in mice. Agomelatine dose not have any antioxidant effects on parameters of oxidative stress produced by Pentylenetetrazole (PTZ) or Picrotoxin (PTX) induced seizure models when compared to controls[3].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : 0.1 mg/mL (insoluble)
DMSO : 90mg/mL (321.7mM)


关键字: S-20098 Hydrochloride | Agomelatine Hydrochloride | S 20098 Hydrochloride | S20098 Hydrochloride

相关产品: glycine | Piromelatine | ACH-000143 | Luzindole | Ramelteon | 4-P-PDOT | 8-M-PDOT | S26131 | Tasimelteon

相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Approved Drug Library | FDA-Approved & Pharmacopeia Drug Library | Clinical Compound Library | Bioactive Compounds Library Max | Antidepressant Compound Library | Inhibitor Library | EMA Approved Drug Library | Bioactive Compound Library

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