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Eur J Pharmacol. 1976 Mar;36(1):231-5.

Butyrophenone influences on the opiate receptor.

Abstract

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.

PMID:
1261596
DOI:
10.1016/0014-2999(76)90277-6
[Indexed for MEDLINE]

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