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Agomelatine

CAS No. : 138112-76-2

MCE 國際站：Agomelatine

產(chǎn)品活性：Agomelatine (S-20098) 是一種 MT1 和 MT2 受體的特異性激動劑，對 CHO-hMT1，HEK-hMT1，CHO-hMT2，HEK-hMT2 的 K_i 分別為 0.1，0.06，0.12 和 0.27 nM。Agomelatine 還是一種選擇性的 5-HT2C 受體拮抗劑，在天然 (豬) 和克隆的人 5-HT2C 受體中 pK_i 分別為 6.4 和 6.2。

研究領(lǐng)域：GPCR/G Protein  |  Neuronal Signaling  |  Metabolic Enzyme/Protease

作用靶點：Melatonin Receptor  |  5-HT Receptor  |  Endogenous Metabolite

In Vitro: 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).
Agomelatine (S20098) also interacts with h5-HT2B receptors (6.6), whereas Agomelatine 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.

In Vivo: 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.

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