Correlation of inhibitory potencies of putative antagonists for sigma receptors in brain and spleen.
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.
D000818:Animals; D014150:Antipsychotic Agents / Q000494:pharmacology; D001923:Brain Chemistry; D002227:Carbazoles / Q000494:pharmacology; D006168:Guinea Pigs; D006220:Haloperidol / Q000494:pharmacology; D066298:In Vitro Techniques; D007546:Isoquinolines / Q000494:pharmacology; D008297:Male; D010620:Phenazocine / Q000031:analogs & derivatives / Q000494:pharmacology; D010879:Piperazines / Q000494:pharmacology; D011743:Pyrimidines / Q000494:pharmacology; D011957:Receptors, Opioid / Q000032:analysis / Q000187:drug effects; D017480:Receptors, sigma; D013154:Spleen / Q000032:analysis*; D014316:Tritium
D014150:Antipsychotic Agents; D002227:Carbazoles; D007546:Isoquinolines; D010879:Piperazines; D011743:Pyrimidines; D011957:Receptors, Opioid; D017480:Receptors, sigma; D014316:Tritium; C050408:alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazine butanol; C012134:SK&F 10047; C051009:HR 375; C034931:rimcazole; D010620:Phenazocine; D006220:Haloperidol