Uses
BMY 14802 Hydrochloride was studied to be a potential atypical antipsychotic agent.
Biological Activity
Potent sigma receptor antagonist (IC 50 = 112 nM) with modest to weak affinity for 5-HT 1A and α 1 receptors. Antipsychotic following oral administration and acts via indirect modulation of central dopaminergic systems.
in vitro
bmy 14802 has its most potent binding at the sigma binding site, with some degree of serotonin subtype 1a and negligible dopamine receptor binding [1].
in vivo
bmy 14802 is atypical of standard neuroleptics in that it does not induce catalepsy in rats. in addition, it has been shown to have efficacy in animal models of psychosis [1].
IC 50
112 nm for (+)-[3h]-3-ppp
References
[1] gewirtz gr, gorman jm, volavka j, macaluso j, gribkoff g, taylor dp, borison r. bmy 14802, a sigma receptor ligand for the treatment of schizophrenia. neuropsychopharmacology. 1994 feb;10(1):37-40.
