SB 243213 hydrochloride is an orally active, selective and high-affinity antagonist of 5-hydroxytryptamine (5-HT)2Creceptor(pKi of 9.37 and a pKb of 9.8).It has improved anxiolytic profile and has the potential for schizophrenia and motor disorders.
SB 243213 dihydrochloride is an orally active, selective and high-affinity antagonist of 5-hydroxytryptamine (5-HT)2Creceptor(pKi of 9.37 and a pKb of 9.8 for human 5-HT2Creceptor).
3-Hydroxy agomelatine D3 is a deuterium labeled 3-Hydroxy agomelatine. 3-Hydroxy agomelatine is an Agomelatine metabolite and a 5-HT2Creceptor antagonist (IC50: 3.2 μM; Ki: 1.8 μM).
Flumexadol is a selective and affinity 5-HT2Creceptor agonist with a Ki of 25 nM for the (+)-enantiomer of Flumexadol, and is 40-fold selective over the 5-HT2A receptor. Flumexadol is an orally active non-narcotic analgesic.
7-Desmethyl-3-hydroxyagomelatine is a metabolite of Agomelatine and has less activity than Agomelatine. Agomelatine is a melatonergic (MT1 and MT2) agonist and 5-HT2C antagonist.
TIK-301 is a chlorinated melatonin derivative and a potent, high-affinity, and orally active melatonin MT1 and MT2 receptors agonist (Kis: 0.081 nM and 0.042 nM, respectively). TIK-301 is also a 5-HT2B 5-HT2Creceptor antagonist with antidepressant action. TIK-301 has the potential for sleep disorders and other circadian rhythm disorders treatment.
Agomelatine (S-20098) L(+)-Tartaric acid is a specific agonist of MT1 and MT2 receptors (Kis: 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2). It also is a selective 5-HT2Creceptor antagonist (pKis: 6.4 and 6.2 at native (porcine) and cloned (human) 5-HT2Creceptors).