Tasimelteon is a melatonin (MT) receptor agonist.1 It selectively binds MT1 and MT2 receptors (Kis = 0.304 and 0.069 nM, respectively, in NIH3T3 cells expressing the recombinant human receptors) over a panel of 160 additional receptors and enzymes at 10 ?M. Tasimelteon inhibits forskolin-induced cAMP accumulation with EC50 values of 0.79 and 1 nM in NIH3T3 cells expressing the MT1 or MT2 receptor, respectively. Formulations containing tasimelteon have been used in the treatment of non-24-hour sleep-wake disorder.
1.Lavedan, C., Forsberg, M., and Gentile, A.J.Tasimelteon: A selective and unique receptor binding profileNeuropharmacology91142-147(2015)