Agomelatine hydrochloride (C09-1101-524)

Agomelatine hydrochloride (S-20098 hydrochloride) is a specific agonist of MT1 and MT2 receptors with K i s of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively Agomelatine hydrochloride is a selective 5-HT2C receptor antagonist with pK i s of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively .In VitroAgomelatine (S 20098) acts as a full agonist of MT1 and MT2 receptors with EC 50 s 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 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoAgomelatine (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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.), respectivelyDosage: 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. Did not have any antioxidant effects on parameters of oxidative stress produced by PTX- or PTZ-induced seizure models when compared to controls.Form:SolidIC50& Target:5-HT 2C Receptor 6.4 (pKi, native porcine) 5-HT 2C Receptor 6.2 (pKi, human) hMT1 0.1 (Ki, CHO Cells) hMT1 0.06 (Ki, HEK Cells) hMT2 0.12 (Ki, CHO Cells) hMT2 0.27 (Ki, HEK Cells). Specification: 0.99 Molecular Formula: C15H18ClNO2 Molecular Weight: 279.76 PubChem CID: 66980040 Isomeric SMILES: CC(=O)NCCC1=CC=CC2=C1C=C(C=C2)OC.Cl