Description | A dopamine receptor antagonist and 5-HT1A partial agonist; binds to dopamine D1, D2, D3, D4, and D5 receptors (Kis = 5.1, 11.6, 24, 1,450, and 5.8 nM, respectively) as well as 5-HT1A, 5-HT2B, α2C-ARs, and σ2 receptors in a radioligand binding assay (Kis = 143, 226, 215, and 53 nM, respectively); inhibits dopamine-induced cAMP accumulation in HEK293 cells expressing dopamine D1, D2, and D5 receptors (IC50 = 20.5, 128, and 27 nM, respectively); inhibits forskolin-induced cAMP production in CHO cells expressing rat 5-HT1A receptors (EC50 = 1.2 µM); increases dopamine neuron firing rates, the number of spikes in bursts, and the amplitude of slow oscillations in the rat VTA at 1 mg/kg; inhibits amphetamine- and phencyclidine-induced locomotor activity in rats (ED50s = 2.4 and 6.5 mg/kg, respectively) |