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

@article{Michel1985BindingOA,
  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},
  year={1985},
  volume={7 4},
  pages={175-7}
}
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

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