Analgesic activity of the naturally occurring heptapeptide [Met]enkephalin-Arg6-Phe7

Proc Natl Acad Sci U S A. 1980 Sep;77(9):5512-4. doi: 10.1073/pnas.77.9.5512.

Abstract

[Met]Enkephalin-Arg6-Phe7 is an opiate-like peptide normally found in the the adrenal gland and brain that has analgesic (antinociceptive) activity when administered directly into the cerebral ventricles of mice. On a molar basis, [Met]-enkephalin-Arg6-Phe7, with a median effective dose (ED50) of 38.5 nmol/mouse, is 8 times more potent than [Met]enkephalin. As with [Met]enkephalin, analgesic activity is blocked by naloxone and intravenous administration does not produce characteristic opiate effects in tests for analgesic, antidiuretic, or antidiarrheal activity. These findings suggest that [Met]enkephalin-Arg6-Phe7 may be at least as important as the enkephalins in the postulated enkephalin system mediating pain and analgesia.

Publication types

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

MeSH terms

  • Analgesics*
  • Animals
  • Diarrhea / drug therapy
  • Diuresis / drug effects
  • Dose-Response Relationship, Drug
  • Endorphins / pharmacology*
  • Enkephalin, Methionine* / analogs & derivatives*
  • Enkephalins / administration & dosage
  • Enkephalins / antagonists & inhibitors
  • Enkephalins / pharmacology*
  • Injections, Intravenous
  • Injections, Intraventricular
  • Male
  • Mice
  • Naloxone / pharmacology
  • Rats

Substances

  • Analgesics
  • Endorphins
  • Enkephalins
  • Naloxone
  • Enkephalin, Methionine
  • enkephalin-Met, Arg(6)-Phe(7)-