Binding of a new opiate antagonist, nalmefene, to rat brain membranes.

  title={Binding of a new opiate antagonist, nalmefene, to rat brain membranes.},
  author={Mary Michel and Gordon T. Bolger and Ben Avi Weissman},
  journal={Methods and findings in experimental and clinical pharmacology},
  volume={7 4},
Nalmefene (6-methylene-naltrexone) is a potent, orally active, opiate antagonist. IC50's were obtained for nalmefene, naloxone and naltrexone using radiolabelled prototype ligands for mu, kappa and delta receptors in homogenates of rat brain minus cerebellum. Nalmefene antagonized the bindings of [3H]-dihydromorphine, [3H]-ethylketocyclazocine and [3H]-D-ala-D-leu enkephalin with IC50's in the low nanomolar range. At the central mu receptor, nalmefene bound with an IC50 of 1.0 nM, equal to that… CONTINUE READING


Publications citing this paper.
Showing 1-10 of 30 extracted citations

Drugs of abuse: chemistry, pharmacology, immunology, and AIDS. Introduction.

NIDA research monograph • 1990
View 3 Excerpts
Highly Influenced

Nalmefene for the management of alcohol dependence: review on its pharmacology, mechanism of action and meta-analysis on its clinical efficacy.

European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology • 2016
View 5 Excerpts
Highly Influenced

The role of the opioid system in alcohol dependence.

Journal of psychopharmacology • 2014
View 7 Excerpts
Highly Influenced

Similar Papers

Loading similar papers…