The proenkephalin A fragment metorphamide shows supraspinal and spinal opioid activity in vivo

A. Dray, T. P. Davis

Research output: Contribution to journalArticle

6 Scopus citations

Abstract

Metorphamide (Tyr-Gly-Gly-Phe-Met-Arg-Arg-Val-NH2) a novel amidated octapeptide fragment of proenkephalin A was synthesized, purified and subsequently shown to inhibit the reflex contractions of the rat urinary bladder following intracerebroventricular and spinal intrathecal microinjections. The effects of metorphamide were consistently antagonized by naloxone but not by the δ-opioid receptor antagonist ICI 174,864. Comparison of metorphamide with other proenkephalin A fragments suggested that the activity of this peptide was not due to in vivo processing to other active fragments. These data suggest that metorphamide has potent in vivo μ-opioid activity but little δ-opioid receptor activity.

Original languageEnglish (US)
Pages (from-to)217-221
Number of pages5
JournalPeptides
Volume6
Issue number2
DOIs
StatePublished - Jan 1 1985

Keywords

  • HPLC
  • Metorphamide
  • Mu, kappa, delta receptors
  • Peptide synthesis
  • Proenkephalin A
  • Rat urinary bladder
  • Reflex contractions

ASJC Scopus subject areas

  • Biochemistry
  • Physiology
  • Endocrinology
  • Cellular and Molecular Neuroscience

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