Butyrophenone influences on the opiate receptor

Research output: Contribution to journalArticle

Abstract

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
Volume36
Issue number1
DOIs
StatePublished - 1976

Fingerprint

Opiate Alkaloids
Butyrophenones
Opioid Receptors
Antipsychotic Agents
Benperidol
Dextropropoxyphene
Pimozide
Meperidine
Structure-Activity Relationship
Naloxone
Benzene
Inhibitory Concentration 50

Keywords

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

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

Cite this

Butyrophenone influences on the opiate receptor. / Creese, Ian; Feinberg, Andrew P; Snyder, Solomon H.

In: European Journal of Pharmacology, Vol. 36, No. 1, 1976, p. 231-235.

Research output: Contribution to journalArticle

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