Contractile effect of morphine and related opioid alkaloids, beta-endorphin and methionine enkephalin on the isolated colon from Long Evans rats

British Journal of Pharmacology
J P Huidobro-Toro, E L Way

Abstract

1 Morphine and related synthetic surrogates as well as beta-endorphin and methionine enkephalin caused a contractile response of the longitudinal musculature of the terminal colon of Long Evans rats.2 The muscular contraction caused by the narcotic analgesics exhibited stereospecificity, with levorphanol being about 50 times more potent than dextrorphan and (-)-methadone 4 times more potent than (+)-methadone. In addition, the rank order in potency of a homologous series of N-alkyl substituted norketobemidones demonstrated that the activity of these compounds in eliciting contractile responses corresponded to that for analgesic efficacy in the rat and also correlated to the ability of these derivatives to inhibit the muscular twitch evoked by electrical stimulation of the guinea-pig ileum.3 Naloxone blocked the contractile response of the opiates following competitive kinetics; the naloxone pA(2) values for morphine, etorphine, levorphanol and methadone were very close, in spite of the marked differences in potency of these agents.4 The contractile effect of morphine on the rat colon was abolished by incubation of the tissues with tetrodotoxin 2.0 x 10(-7) M or by decreasing the external Ca(2+) level 100 fold. Increasing the ex...Continue Reading

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Citations

Sep 1, 1986·Veterinary Research Communications·L Ooms, A Degryse
Nov 5, 1982·European Journal of Pharmacology·J J Galligan, T F Burks
Aug 5, 1983·European Journal of Pharmacology·J S LiuE L Way
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