2-Phenylmelatonin

2-Phenylmelatonin is a melatonin 1 (MT1) and MT2 receptor mixed partial agonist and antagonist.{53155,30339,58713} It selectively binds to MT1 and MT2 receptors (Kis = 0.02 and 0.09 nM, respectively, in HEK293 cells expressing the human receptors) over the MT3 receptor (Ki = 33 nM in hamster brain membranes).{53155} 2-Phenylmelatonin induces [35S]GTPyS binding to NIH3T3 cell membranes expressing the human MT2 receptor (EC50 = 0.058 nM).{30339} It induces contractions (EC50 = 0.5 nM) and inhibits melatonin-induced contractions in isolated guinea pig proximal colon strips when used at a concentration of 0.1 nM.{58713} 2-Phenylmelatonin reduces intraocular pressure in rabbits (pD2 = 8.7).{58714}