IC50: 112 nM for (+)-[3H]-3-PPP
The theoretical role of sigma receptors in psychosis has led to the discovery of selective sigma receptor ligands as potential antipsychotic agents. BMY 14802 is a sigma receptor ligand.
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].
Clinical trial: After 1 week of single-blind placebo treatment, 28 patients were treated with BMY 14802 (up to 3000 mg/day) for up to 4 weeks. However, there was no significant improvement in psychiatric symptoms. There were no changes in involuntary movements, as measured by the Abnormal Involuntary Movement Scale, or in extrapyramidal symptoms as measured by the Simpson-Angus Scale [1].
Reference:
[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.