Trebenzomine (CI-686) is a centrally acting psychotropic drug structurally distinct from currently available drugs. Preclinical studies indicate that trebenzomine, unlike most psychotropic drugs, has both neuroleptic and stimulant profiles. Stimulant properties of trebenzomine include potentiation of methamphetamine-induced self-stimulation. Neuroleptic properties of trebenzomine include reduction of septal hyperirritability, suppression of conditioned avoidance behavior, blockade of apomorphine-induced emesis in dogs, and elevation of brain homovanillic acid (HVA). Trebenzomine's effect on dopamine (DA) metabolism appears to be related more to the presynaptic release of DA rather than by blockade of postsynaptic DA receptors. Unique preclinical profile suggests a mechanism of action other than dopamine antagonism which could have implications regarding current thinking on the pathophysiology of schizophrenia.