Agomelatine

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MT1 (Ki=0.1nM) 和 MT2 (Ki=0.12nM) 褪黑激素受体激动剂，以及 5-HT2C (Ki=631nM) 受体拮抗剂。

A melatonin receptor agonist of MT1 (Ki=0.1nM) and MT2 (Ki=0.12nM), and a 5-HT2C (Ki=631nM) receptor antagonist; has no effect on monoamine uptake and no affinity for adrenergic, histaminergic, cholinergic, dopaminergic and benzodiazepine receptors, nor other serotonergic receptors; a melatonergic antidepressant treatment of major depressive disorder with relatively favorable side effect profile.Depression Approved(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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Animal Model:Female Swiss mice (20-30 g) were administered PTZ (85 mg/kg, i.p.), PTX (7 mg/kg, i.p.), strychnine (75 mg/kg, i.p.), Pilocarpine (400 mg/kg, i.p.), respectively.Dosage:25, 50, or 75 mg/kg Administration:Administered intraperitoneally (i.p.)Result:All dosages showed a significant decrease in thiobarbituric acid reactive substances (TBARS) levels and nitrite content in all brain areas when compared to controls in the Pilocarpine induced seizure model.All dosages decreased TBARS levels in all brain areas, and at low doses (25 or 50 mg/kg) decreased nitrite contents, but only at 25 or 50 mg/kg showed a significant increase in catalase activity in three brain areas when compared to controls in the Strychnine-induced seizure model.

S-20098

GPCR/G Protein

Melatonin Receptor

5-HT

Neurological Disease

Depression

138112-76-2

243.301

C15H17NO2

>98% (HPLC)

10 mM in DMSO

CC(=O)NCCC1=CC=CC2=C1C=C(C=C2)OC

Acetamide, N-[2-(7-methoxy-1-naphthalenyl)ethyl]-

(-20℃)

With Ice Pack

≥ 2 years