Phenyl??substituted Normethadones: Synthesis and Pharmacology

…, JH Poupaert, J Cumps, C Moussebois…

Index: Mbela; Poupaert; Cumps; Moussebois; Haemers; Borloo; Dumont Journal of Pharmacy and Pharmacology, 1995 , vol. 47, # 3 p. 237 - 242

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Citation Number: 2

Abstract

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 p-opioid receptor and that the P subsite has a well-defined cavity shape of stringent ...