Motility effects of opioid peptides in dog intestine.
Six opioid peptides, like morphine, were found to produce dose-dependent contractions of dog isolated intestine when administered as intraarterial boluses. The increases in incidence and amplitude of intestinal contractions were antagonized by naloxone. The rank order of potency of the opioid agonists tested was D-Ala2-met-enkephalinamide greater than D-Ala2-leu-enkephalinamide greater than met-enkephalin greater than beta-endorphin 1-31 greater than morphine greater than morphiceptin greater than dynorphin 1-13. The contractions induced by two opioid agonists displayed differential sensitivity to blockade by tetrodotoxin (TTX). Met-enkephalin was barely affected by concentrations of TTX that markedly reduced responses to morphiceptin. Some portion of the motility effect of metenkephalin may be exerted directly on intestinal smooth muscle.
D000818:Animals; D004285:Dogs; D004399:Dynorphins; D004723:Endorphins / Q000494:pharmacology*; D004743:Enkephalin, Leucine / Q000031:analogs & derivatives / Q000494:pharmacology; D016308:Enkephalin, Leucine-2-Alanine / Q000031:analogs & derivatives*; D004744:Enkephalin, Methionine / Q000031:analogs & derivatives / Q000494:pharmacology; D005260:Female; D005769:Gastrointestinal Motility / Q000187:drug effects*; D008297:Male; D009020:Morphine / Q000494:pharmacology; D010446:Peptide Fragments / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013779:Tetrodotoxin / Q000494:pharmacology; D001615:beta-Endorphin
D004723:Endorphins; D010446:Peptide Fragments; D013779:Tetrodotoxin; D004744:Enkephalin, Methionine; D004743:Enkephalin, Leucine; D001615:beta-Endorphin; C013801:enkephalin-Met, Ala(2)-; D016308:Enkephalin, Leucine-2-Alanine; C030279:enkephalinamide-Leu, Ala(2)-; C026843:dynorphin (1-13); D004399:Dynorphins; D009020:Morphine; C028889:morphiceptin