3-Hydroxy agomelatine is a major metabolite of Agomelatine (IC50 of 3.2 μM and a Ki of 1.8 μM). Agomelatine is a potent antidepressant acting as 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. Agomelatine L(+)-Tartaric acid is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor. It is a unique antidepressant and is developed for treatment of major depressive disorder (MDD). It shows low affinities to cloned human 5-HT2A and 5-HT1A. In the in vivo studies, agomelatine causes increase of dopamine and noradrenaline levels via blocking the inhibitory input of 5-HT2C.
纯度:≥98%
CAS:166526-99-4