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PMID: 6933569 Published · ppublish English Journal Article Research Support, Non-U.S. Gov't Research Support, U.S. Gov't, P.H.S.

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

Inturrisi CE, Umans JG, Wolff D, Stern AS, Lewis RV, Stein S, Udenfriend S

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.

MeSH Terms
Analgesics Animals Diarrhea/drug therapy Diuresis/drug effects Dose-Response Relationship, Drug Endorphins/pharmacology Enkephalin, Methionine/analogs & derivatives Enkephalins/administration & dosage,antagonists & inhibitors,pharmacology Injections, Intravenous Injections, Intraventricular Male Mice Naloxone/pharmacology Rats
Chemicals
Analgesics Endorphins Enkephalins Naloxone Enkephalin, Methionine enkephalin-Met, Arg(6)-Phe(7)-
Authors & Affiliations
7 authors, click to expand affiliations / ORCID
Inturrisi C E
Umans J G
Wolff D
Stern A S
Lewis R V
Stein S
Udenfriend S
References (13)
13 references, click to expand
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Article Info
Journal
Proceedings of the National Academy of Sciences of the United States of America
Abbr.
Proc Natl Acad Sci U S A
ISSN
0027-8424
Published
1980-09-00
Pages
5512-4
Language
English
Region
United States
NLM ID
7505876
PMCID
PMC350091
Subset
IM
Grants
NIDA NIH HHS · DA-01457 · United States
NIGMS NIH HHS · GM-26145 · United States
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