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 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.
D000603:Amino Acids, Sulfur / Q000494:pharmacology*; D000698:Analgesia; D000818:Animals; D004744:Enkephalin, Methionine / Q000494:pharmacology; D004745:Enkephalins / Q000502:physiology*; D007930:Leucine / Q000031:analogs & derivatives* / Q000494:pharmacology; D008297:Male; D051379:Mice; D010146:Pain / Q000503:physiopathology*; D011480:Protease Inhibitors / Q000494:pharmacology*; D011957:Receptors, Opioid / Q000502:physiology*; D017450:Receptors, Opioid, mu; D015244:Thiorphan; D008625:Tiopronin / Q000031:analogs & derivatives / Q000494:pharmacology*
D000603:Amino Acids, Sulfur; D004745:Enkephalins; D011480:Protease Inhibitors; D011957:Receptors, Opioid; D017450:Receptors, Opioid, mu; D004744:Enkephalin, Methionine; D015244:Thiorphan; D008625:Tiopronin; D007930:Leucine; C012211:ubenimex