The opioid kappa-selective compound U-50,488H does not inhibit intestinal propulsion in rats.
The selective kappa-compound U-50,488H, at doses producing strong central pharmacological effects (0.5-32 mg kg-1 i.p.) did not delay the intestinal transit of a charcoal meal and had little or no antagonist action against morphine-induced constipation. It appears that kappa-opioid receptors are probably not involved in the mechanisms responsible for opioid-induced constipation.
D019900:3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer; D000818:Animals; D005769:Gastrointestinal Motility / Q000187:drug effects*; D008297:Male; D009020:Morphine / Q000494:pharmacology; D009619:Nociceptors / Q000187:drug effects; D011759:Pyrrolidines / Q000494:pharmacology*; D051381:Rats; D011957:Receptors, Opioid / Q000187:drug effects*; D017473:Receptors, Opioid, kappa
D011759:Pyrrolidines; D011957:Receptors, Opioid; D017473:Receptors, Opioid, kappa; D019900:3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer; D009020:Morphine