1176316-99-6

Agomelatine hydrochloride (S-20098 hydrochloride) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively[1]. Agomelatine hydrochloride is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively[2].

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)

[1] Audinot V, et al. New selective ligands of human cloned melatonin MT1 and MT2 receptors. Naunyn Schmiedebergs Arch Pharmacol. 2003 Jun;367(6):553-61. DOI:10.1007/s00210-003-0751-2
[2] Millan MJ, 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 pathways. J Pharmacol Exp Ther. 2003 Sep;306(3):954-64. DOI:10.1124/jpet.103.051797
[3] Aguiar CC, et al. Effects of agomelatine on oxidative stress in the brain of mice after chemically induced seizures. Cell Mol Neurobiol. 2013 Aug;33(6):825-35. DOI:10.1007/s10571-013-9949-0