Butyrophenone influences on the opiate receptor

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65 Scopus citations


Interaction of neuroleptic drugs with the opiate receptor was investigated by inhibition of the stereospecific binding of 3H-naloxone. Benperidol and pimozide, with IC50's of 0.3-0.5 μM, 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.

Original languageEnglish (US)
Pages (from-to)231-235
Number of pages5
JournalEuropean Journal of Pharmacology
Issue number1
StatePublished - Mar 1976


  • Butyrophenone
  • Neuroleptic
  • Opiate receptor
  • Pehnothiazine
  • Structure-activity

ASJC Scopus subject areas

  • Pharmacology


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