Pain control by endogenous enkephalins is mediated by mu opioid receptors

The analgesic effects of bestatin and thiorphan, two enzymatic inhibitors protecting endogenous enkephalins from their degradation, and those of DAGO and deltakephalin, respectively mu and delta opioid peptides, are assessed on the electrical stimulation test of the mouse tail. The relative analgesi...

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Published inLife sciences (1973) Vol. 33 Suppl 1; p. 685
Main Authors Chaillet, P, Coulaud, A, Fournié-Zaluski, M C, Gacel, G, Roques, B P, Costentin, J
Format Journal Article
LanguageEnglish
Published Netherlands 1983
Subjects
Amino Acids, Sulfur - pharmacology
Analgesia
Animals
Enkephalin, Methionine - pharmacology
Enkephalins - physiology
Leucine - analogs & derivatives
Leucine - pharmacology
Male
Mice
Pain - physiopathology
Protease Inhibitors - pharmacology
Receptors, Opioid - physiology
Receptors, Opioid, mu
Thiorphan
Tiopronin - analogs & derivatives
Tiopronin - pharmacology
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Summary:The analgesic effects of bestatin and thiorphan, two enzymatic inhibitors protecting endogenous enkephalins from their degradation, and those of DAGO and deltakephalin, respectively mu and delta opioid peptides, are assessed on the electrical stimulation test of the mouse tail. The relative analgesic potency of DAGO and deltakephalin is in good agreement with their relative potency on mu pharmacological assays: inhibition of electrically-induced contractions of guinea-pig ileum, displacement of 3H DAGO on rat brain. Finally, the analgesic effects of DAGO, deltakephalin and bestatin + thiorphan, are antagonized by the mu antagonist naloxone with similar pA2, and they are not modified by the delta antagonist ICI 154, 129. We conclude that only mu and not delta receptors are involved in the analgesic effects of enkephalins.
ISSN:0024-3205
DOI:10.1016/0024-3205(83)90595-7