Beta-endorphin-(1-27) is a naturally occurring antagonist to etorphine-induced analgesia

Proc Natl Acad Sci U S A. 1985 May;82(10):3178-81. doi: 10.1073/pnas.82.10.3178.

Abstract

The potent opioid peptide beta-endorphin is found in the brain and pituitary with two related fragments, beta-endorphin-(1-27) and beta-endorphin-(1-26). The fragments retain substantial opioid-receptor binding activity but are virtually inactive analgesically. beta-Endorphin-(1-27) inhibits beta-endorphin-induced and etorphine-induced analgesia when coinjected intracerebroventricularly into mice. Antagonism by competition at the same site(s) is suggested from parallel shifts of the dose-response curves of etorphine or beta-endorphin in the presence of beta-endorphin-(1-27). Its potency is 4-5 times greater than that of the opiate antagonist naloxone. beta-Endorphin-(1-26) does not antagonize the antinociceptive action of etorphine or beta-endorphin in doses up to 500 pmol per animal.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Binding, Competitive
  • Dose-Response Relationship, Drug
  • Endorphins / metabolism
  • Endorphins / pharmacology*
  • Etorphine / antagonists & inhibitors*
  • Etorphine / metabolism
  • Male
  • Mice
  • Morphinans / antagonists & inhibitors*
  • Naloxone / pharmacology
  • Pain / physiopathology*
  • Peptide Fragments / metabolism
  • Peptide Fragments / pharmacology*
  • Receptors, Opioid / metabolism
  • beta-Endorphin*

Substances

  • Endorphins
  • Morphinans
  • Peptide Fragments
  • Receptors, Opioid
  • Naloxone
  • Etorphine
  • beta-Endorphin
  • beta-endorphin (1-27)