JNJ-37822681 is a dopamine D2L receptor antagonist (Ki = 0.158 ?M).1 It is selective for dopamine D2L receptors over dopamine D1 and D3, α1-adrenergic, and histamine H1 receptors, and the serotonin (5-HT) receptor subtypes 5-HT2A and 5-HT2C in radioligand binding assays (Kis = >3, 1.159, >5, 4.931, 2.896, and >4 ?M, respectively). JNJ-37822681 inhibits apomorphine-induced stereotypy and D-amphetamine-induced hyperlocomotion in rat models of psychosis (ED50s = 0.19 and 1 mg/kg, respectively).
1.Langlois, X., Megens, A., Lavreysen, H., et al.Pharmacology of JNJ-37822681, a specific and fast-dissociating D2 antagonist for the treatment of schizophreniaJ. Pharmacol. Exp. Ther.342(1)91-105(2012)