Agomelatine hydrochloride (E6011-GRP)

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. It is also a selective antagonist of 5-HT2C receptors with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively. Blockade of these receptors enhances adrenergic and dopaminergic transmission in the frontocortical regions.