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
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