Binding of a new opiate antagonist, nalmefene, to rat brain membranes
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DOI:
文献链接: https://pubmed.ncbi.nlm.nih.gov/2991678
其他信息:
PMID: 2991678
作者: M E Michel; G Bolger; B A Weissman; M E Michel; M E Michel; ...
摘要: 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 ...
