Characterization of the opiate receptor in the guinea-pig ileal mucosa

James F. Kachur, Richard J. Miller*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

36 Scopus citations

Abstract

Several opioid peptides and narcotic drugs reduced transepithelial potential difference (PD) and short circuit current (Isc) in guinea-pig ileal mucosa measured in vitro in Ussing chambers. [D-Ala2,D-Leu5]enkephalin was the most potent peptide tested. Enkephalin analogues with altered C-terminal amino acids were less potent, as were ß-endorphin and dermorphin. Etorphine produced potent effects whereas morphine and SKF 10,047 were inactive. Ethylketazocine produced a biphasic dose-response curve. When added by themselves diprenorphine and naloxone produced small increases in Isc. This effect was not seen when Cl- and HCO3- in the Ringer were replaced by SO42-. Diprenorphine and naloxone were able to shift the dose response curves for all agonists to the right, with the exception of that for ethylketazocine. Diprenorphine was a more potent antagonist than naloxone. SKF 10,047 also acted as a pure antagonist. Morphine and ethylketazocine had no antagonist effects. It is concluded that the opiate receptor in the guinea-pig ileal mucosa is similar to a δ-opiate receptor as defined by ligand binding studies, but that some differences also exist.

Original languageEnglish (US)
Pages (from-to)177-183
Number of pages7
JournalEuropean Journal of Pharmacology
Volume81
Issue number2
DOIs
StatePublished - Jul 9 1982

Keywords

  • Enkephalins
  • Ileal mucosa
  • Intestinal secretion
  • Opiate antagonists
  • δ-Receptor

ASJC Scopus subject areas

  • Pharmacology

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