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Phenyl-substituted normethadones: synthesis and pharmacology
T K Mbela1, J H Poupaert, J Cumps
1Department of Pharmaceutics and Drug Analysis, Faculty of Pharmacy, University of Kinshasa, Zaire.
The Journal of Pharmacy and Pharmacology
|March 1, 1995
Abstract:
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.