Pharmacological characterization of opiate physical dependence in the isolated ileum of the guinea-pig

Br J Pharmacol. 1981 Aug;73(4):859-66. doi: 10.1111/j.1476-5381.1981.tb08739.x.

Abstract

1 Physical dependence was produced in ilea from naive guinea-pigs by exposure of the tissue to different opiates for logarithmically-spaced periods of time (20-320 min). The responsiveness of the tissue to naloxone, as indicated by a strong contracture of the ileum, was enhanced in contrast to that found in intestines not exposed to opiates. 2 The dose-response curves to naloxone obtained in tissues individually exposed to different opiates showed that their relative potency in increasing sensitivity to naloxone was as follows: levorphan greater than morphine greater than Met-enkephalin greater than nalorphine greater than pentazocine. 3 The naloxone-induced response was dose-dependent and was directly related to the opiate concentration and length of exposure. 4 Dextrorphan the inactive isomer of levorphan, did not increase the responsiveness of the tissues to the narcotic antagonist, indicating that the phenomenon is stereospecific. 5 The naloxone-induced contraction in ilea exposed for 320 min to morphine (1 x 10(-6)M) was not prevented or suppressed by the administration of a large dose of morphine (1 x 10(-5)M) before or immediately after the naloxone challenge. 6 The evidence presented here shows that a phenomenon resembling in vivo opiate physical dependence can be acutely produced in vitro with pharmacological characteristics similar to other naloxone-induced abstinence effects.

MeSH terms

  • Animals
  • Dose-Response Relationship, Drug
  • Enkephalin, Methionine
  • Enkephalins / pharmacology
  • Guinea Pigs
  • Humans
  • Ileum / drug effects*
  • In Vitro Techniques
  • Levorphanol / pharmacology
  • Male
  • Morphine / pharmacology
  • Nalorphine / pharmacology
  • Naloxone / pharmacology
  • Narcotics*
  • Pentazocine / pharmacology
  • Substance-Related Disorders*
  • Time Factors

Substances

  • Enkephalins
  • Narcotics
  • Levorphanol
  • Naloxone
  • Enkephalin, Methionine
  • Morphine
  • Pentazocine
  • Nalorphine