Correlation of inhibitory potencies of putative antagonists for sigma receptors in brain and spleen

Abstract

The putative sigma receptor antagonists, haloperidol, HR 375, BMY 14802 and BW 234U potently inhibited both [3H]d-N-allylnormetazocine binding to sigma receptors in brain homogenates and [3H]haloperidol binding to sigma receptors in spleen homogenates. An excellent correlation of inhibitory potencies in the two assay systems was obtained. The results support the view that [3H]d-N-allylnormetazocine and [3H]haloperidol both label the same receptor populations, and suggest that sigma antagonists may be useful in elucidating physiological role(s) of sigma receptors in the nervous and immune systems.