A comparison of the effects of 6-beta naltrexol and naltrexone on the consumption of ethanol or sucrose using a limited-access procedure in rats

Pharmacol Biochem Behav. 2002 May;72(1-2):483-90. doi: 10.1016/s0091-3057(02)00721-9.

Abstract

We recently reported that 6-beta naltrexol, the major metabolite of naltrexone in humans, reduced ethanol consumption in rats. Two new experiments were designed to compare 6-beta naltrexol and naltrexone across three dose levels on an ethanol or sucrose baseline using a limited-access procedure in Wistar rats. The results of Experiment 1 showed that both 6-beta naltrexol and naltrexone reduced ethanol consumption across a range of doses. An in vivo assay showed that naltrexone was approximately 25 times more potent than 6-beta naltrexol at comparable ED50 doses. In addition, there was no indication of systematic development of tolerance to the effect of either drug across the 4 days of drug administration. In Experiment 2, both 6-beta naltrexol and naltrexone reduced the consumption of a sucrose solution using a limited-access procedure. The implications of these data for the development of pharmacotherapeutic agents capable of reducing drinking in recovering alcoholics are discussed.

Publication types

  • Comparative Study
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Alcohol Drinking / drug therapy*
  • Animals
  • Dose-Response Relationship, Drug
  • Ethanol / antagonists & inhibitors
  • Ethanol / pharmacology*
  • Male
  • Naltrexone / analogs & derivatives*
  • Naltrexone / pharmacology*
  • Naltrexone / therapeutic use
  • Rats
  • Rats, Wistar
  • Sucrose / antagonists & inhibitors
  • Sucrose / pharmacology*

Substances

  • Ethanol
  • 6 beta-hydroxynaltrexone
  • Sucrose
  • Naltrexone