Tasimelteon

Tasimelteon is a potent Dual Melatonin Receptor Agonist (DMRA). It is used to treat non-24-hour sleep-wake disorder. The Ki values for binding affinity at melatonin receptors MT1 and MT2 receptor are 0.304 and 0.069 nM respectively in CHO–K1 cells. It shows greater affinity for the MT2 receptor which is believed to mediate circadian rhythm phase-shifting. It induces a potent, concentration-dependent inhibition of forskolin-stimulated cAMP accumulation in NIH-3T3 cells stably expressing human MT1 and MT2 receptors with EC₅₀ values of 0.74 nM and 0.1 nM repectively.