PG-01037 is a selective dopamine D3 receptor antagonist (Kis = 0.7, 93, and 375 nM for HEK293 cells expressing human D3, D2, and D4 receptors, respectively). It inhibits quinpirole-induced stimulation of mitogenesis in CHO cells expressing human dopamine D3 receptors (EC50 = 3 nM). PG-01037 (32 mg/kg) reduces progressive-ratio methamphetamine self-administration in rats allowed extended access. It reduces loss of dopaminergic neurons in the substantia nigra pars compacta and improves motor performance in the coat-hanger test in a mouse model of Parkinson''s disease induced by MPTP.