Butyrophenone influences on the opiate receptor.
Interaction of neuroleptic drugs with the opiate receptors was investigated by inhibition of the stereospecific binding of 3H-naloxone. Benperidol and pimozide, with IC50's of 0.3-0.5 muM, were more potent than the classical opiates meperidine and propoxyphene. A systematic structure-activity relationship was evident with the basic opiate structure of a benzene and a piperidine ring preserved in active compounds. No correlation between neuroleptic activity and binding to the opiate receptor was demonstrated.
D000818:Animals; D001544:Benperidol / Q000494:pharmacology; D001562:Benzimidazoles / Q000494:pharmacology; D001921:Brain / Q000378:metabolism; D002090:Butyrophenones / Q000494:pharmacology*; D011431:Dextropropoxyphene / Q000494:pharmacology; D066298:In Vitro Techniques; D008297:Male; D008614:Meperidine / Q000494:pharmacology; D009270:Naloxone / Q000378:metabolism*; D010640:Phenothiazines / Q000494:pharmacology; D010868:Pimozide / Q000494:pharmacology; D051381:Rats; D011955:Receptors, Drug / Q000187:drug effects*; D013329:Structure-Activity Relationship
D001562:Benzimidazoles; D002090:Butyrophenones; D010640:Phenothiazines; D011955:Receptors, Drug; D010868:Pimozide; D009270:Naloxone; D001544:Benperidol; D008614:Meperidine; D011431:Dextropropoxyphene