Opiate receptor binding affected differentially by opiates and opioid peptides

Steven R. Childers, Ian Creese, Adele M. Snowman, Solomon H. Snyder

Research output: Contribution to journalArticle

Abstract

The potencies of various opiates in displacing several 3H-opiates ligands′ binding to rat brain membranes vary depending on the nature of the ligand. Whereas opiate antagonists, as well as the opioid peptides and somes agonists (etorphine, levorphanol and phenazocine) display similar affinities in displacing either 3H-opiate or 3H-methionine enkephalin binding, other agonists (such as morphine and oxymorphone) are considerably (20-50 times) weaker in displacing 3H-enkephalin than 3H-dihydromorphine binding. These agonists also compete for 3H-enkephalin binding with shallow displacement curves, and are greatly weakened in displacing 3H-naloxone binding in the presence of sodium. These agonists differ from the other opiate classes by processing a relatively hydrophilic component in their C-ring moieties which may provide a basis for the differential interactions of drugs with the opiate receptor.

Original languageEnglish (US)
Pages (from-to)11-18
Number of pages8
JournalEuropean Journal of Pharmacology
Volume55
Issue number1
DOIs
StatePublished - Apr 1 1979

Keywords

  • Opiate receptors
  • Opiates
  • Opioid peptides

ASJC Scopus subject areas

  • Pharmacology

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