BMY 14802 was identified as a potential
antipsychotic drug in traditional model systems, and this identification was confirmed in modern behavioral and electrophysiological systems. The
drug appears to be atypical as an
antipsychotic in its lack of activity in models predictive of the potential to produce extrapyramidal side effects and
tardive dyskinesia. Indeed, this suggestion is corroborated by clinical findings to date. The atypical profile of
BMY 14802 extends to its neurochemical actions and appears to find its basis in regionally selective, indirect modulation of the
dopamine system. Furthermore,
BMY 14802 exhibits interactions with sigma binding sites in vitro and in vivo, a notion supported by data from neurophysiological, behavioral, and biochemical investigations.
BMY 14802 also appears to be neuroprotective in some model systems and may have utility in the treatment of
stroke (Boissard et al. 1991).
BMY 14802 appears to interact with 5-HT1A receptors, but this interaction does not seem to contribute significantly to the potential
antipsychotic actions of the
drug. Moreover, the formation of active metabolites of
BMY 14802 does not appear to occur in animals or humans to an extent of physiological or behavioral relevance. If clinically efficacious,
BMY 14802 may treat the symptoms of
schizophrenia by a mechanism novel for
antipsychotic drugs: regionally selective, indirect modulation of dopaminergic systems by specific interaction at sigma sites.