Lumateperone is an atypical antipsychotic.1 It selectively binds to the serotonin (5-HT) receptor subtype 5-HT2A over 5-HT1A and 5-HT2C receptors (Kis = 0.54, 1,480, and 173 nM, respectively). Lumateperone also binds to dopamine D1, D2, and D4 receptors (Kis = 52, 32, and 108 nM, respectively), α1A- and α1B-adrenergic receptors (Kis = 73 and 31 nM, respectively), and the 5-HT transporter (SERT; Ki = 61 nM). It reduces head-twitch behavior induced by the 5-HT2A agonist quipazine in rats (ED50 = 0.12 mg/kg). Formulations containing lumateperone have been used in the treatment of schizophrenia.
1.Li, P., Zhang, Q., Robichaud, A.J., et al.Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disordersJ. Med. Chem.57(6)2670-2682(2014)