Analgesic activity of the naturally occurring heptapeptide [Met]enkephalin-Arg6-Phe7.
Author(s) -
Charles E. Inturrisi,
Jason G. Umans,
David Wolff,
A S Stern,
Randolph V. Lewis,
S Stein,
Sidney Udenfriend
Publication year - 1980
Publication title -
proceedings of the national academy of sciences
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.011
H-Index - 771
eISSN - 1091-6490
pISSN - 0027-8424
DOI - 10.1073/pnas.77.9.5512
Subject(s) - enkephalin , analgesic , (+) naloxone , opiate , opioid peptide , met enkephalin , nociception , neuropeptide , chemistry , opioid , pharmacology , endocrinology , medicine , receptor
[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.
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