Cayman Brexpiprazole

Brexpiprazole is a serotonin (5-HT) and dopamine receptor modulator that has high affinity (K_i = <1 nM) for 5-HT_1A and 5-HT_2A serotonin, dopamine D_2L, and α_1B-, and α_2C-adrenergic receptors in CHO cell membranes expressing the human receptors. It acts as a partial agonist of 5-HT_1A, D_2L, and D₃ receptors (EC₅₀s = 0.49, 4.0, and 2.8 nM, respectively) and an antagonist of 5-HT_2A, 5-HT_2B, as well as α_1B- and α_2C-adrenergic receptors (IC₅₀s = 6.5, 14, 0.66, and 63 nM, respectively) in vitro. In vivo, brexpiprazole dose-dependently reduces conditioned avoidance response (CAR) time, inhibits locomoter hyperactivity induced by apomorphine (Item No. ) and amphetamine, and reverses cognitive defects induced by subchronic PCP administration in rats. It also reduces apomorphine-induced eye blinking in cynomolgus monkeys. Formulations containing brexpiprazole have been used in the treatment of schizophrenia and major depressive disorder.

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