Phenyl-substituted Normethadones - Synthesis and Pharmacology

Mbela, TKN.;Poupaert, Jacques;Cumps, Jean;Moussebois, Claude;Dumont, Pierre;et.al.
(1995) Journal of Pharmacy and Pharmacology — Vol. 47, n° 3, p. 237-242 (1995)

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Authors
  • Mbela, TKN.
    Author
  • Poupaert, JacquesUCLouvain
    Author
  • Cumps, JeanUCLouvain
    Author
  • Moussebois, ClaudeUCLouvain
    Author
  • Dumont, PierreUCLouvain
    Author
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Abstract
Phenyl-substituted normethadone derivatives were synthesized and their affinity (IC50) for opioid receptors was determined by displacement of the specific binding sites of [H-3]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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Mbela, TKN., Poupaert, J., Cumps, J., Moussebois, C., Haemers, A., Borloo, M., & Dumont, P. (1995). Phenyl-substituted Normethadones - Synthesis and Pharmacology. Journal of Pharmacy and Pharmacology, 47(3), 237-242. https://hdl.handle.net/2078.5/83377 (Original work published 1995)