Phenyl-substituted normethadone derivatives were synthesized and their affinity (IC50) for opioid receptors was determined by displacement of the specific binding sites of [3H]sufentanyl on rat brain preparations. Substitution resulted in a decrease of affinity in-vitro. These results suggest that normethadone-like compounds may interact with the P subsite of the mu-opioid receptor and that the P subsite has a well-defined cavity shape of stringent dimensions.
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| http://dx.doi.org/10.1111/j.2042-7158.1995.tb05786.x | DOI Listing |
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Phenyl-substituted normethadones: synthesis and pharmacology.
J Pharm Pharmacol
March 1995
Department of Pharmaceutics and Drug Analysis, Faculty of Pharmacy, University of Kinshasa, Zaire.
Phenyl-substituted normethadone derivatives were synthesized and their affinity (IC50) for opioid receptors was determined by displacement of the specific binding sites of [3H]sufentanyl on rat brain preparations. Substitution resulted in a decrease of affinity in-vitro. These results suggest that normethadone-like compounds may interact with the P subsite of the mu-opioid receptor and that the P subsite has a well-defined cavity shape of stringent dimensions.
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