New developments in opioid receptors ligands
Ronsisvalle, G., Prezzavento,O., Pasquinucci, L., Marrazzo, A., Vittorio, F., Pappalardo, M.S. and Bousquet, E.
Instituto di Chimica Farmaceutica e Tossicologica. Universitą degli Studi di Catania. Viale A. Doria, 6 - Cittą Universitaria. 95125 Catania - Italy.
Ars Pharm.36;(3);433-443, (1995)
Key words: Opioid Agonists and Antagonists, Selective Ligands, Bivalent Ligands, Message-Address HypothesisAbstract
Relevant developments have been achieved in the last twenty years in the search for opioid agonists and antagonists with selectivity for each receptor subpopulation. Recently, new benzomorphan derivatives have been synthesized and compounds with substituted cyclopropylmethyl funcionalities at N-1 position showed high affinity and selectivity for k opioid receptor subpopulations. MPCB and CCB were selected as specific k agonists. The affinity of CCB was two-fold the USO,488H one. Mixed peptide-heterocyclic compounds have been derived from these compounds and important informations on binding processes of k ligands have been obtained.
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