En los últimos veinte años se ha llevado a cabo una intensa investigación sobre la búsqueda de agonistas y antagonistas selectivos de cada subtipo de receptores opiáceos. Recientemente se han sintetizado nuevos derivados benzomorfánicos y compuestos con restos ciclopropilmetílicos sobre N-1 que muestran alta afinidad y selectividad por los receptores kappa. Los compuestos MPCB y CCB se han seleccionado como agonistas específicos kappa. La afinidad de CCB es dos veces mayor que la del compuesto USO,488H. De estos compuestos se han derivado interesantes compuestos con estructura de peptido-heterociclo y se han obtenido importantes informaciones sobre los procesos de binding a los receptores kappa.
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 functionalities at N-1 position showed high affinity and selectivity for κ opioid receptor subpopulations. MPCB and CCB were selected as specific κ 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 κ ligands have been obtained.
New developments in opioid receptors ligands
PREZZAVENTO, Orazio;PASQUINUCCI, Lorella Giuseppina;MARRAZZO, Agostino;
1995-01-01
Abstract
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 functionalities at N-1 position showed high affinity and selectivity for κ opioid receptor subpopulations. MPCB and CCB were selected as specific κ 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 κ ligands have been obtained.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.