Investigaciones actuales en ligandos de receptores opiáceos
Abstract
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-l que muestran alta afinidad y selectividad por los
receptores K . Los compuestos MPCB y CCB se han seleccionado como agonistas específicos
- 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 peptidoheterocido
y se han obtenido importantes informaciones sobre los procesos de binding a
los receptores K.
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References
T. (1994): "Phannacological Characterization ofthe cloned K-, 0-, and J.l- opioid receptors",
Molecular Pharmacol., 45:330-334.
PORTOGHESE, P. S., LARSON, D. L., SA YRE, L. M., FRIES, D. S. and TAKEMORI,
A. E. (1980): "A novel opioid receptor site directed alkylating agent with irreversible
narcotic antagonistic and reversible agonistic activities", J. Med. Chem., 23:233-234.
PORTOGHESE, P. S., LIPKOWSKI, A. and TAKEMORI, A. E. (1987): "Binaltorphirnine
and norbinaltorphirnine, potent and selective K-opioid receptor antagonists", Lije Sci.,
40:1287-1292.
BURKE, T. R., Jr., BAJWA, B. S., JACOBSON, A. E., RICE, K. C., STREATY, R. A.
and KLEE, W. A. (1984): "Probes for Narcotic receptor mediated phenomena. 7. Synthesis
. and phannacological properties of irreversible ligand specific for J.l or o opiate receptors",
J. Med. Chem., 27:1570-1574.
EREZ, M., TAKEMORI, A. E. and PORTOGHESE, P. S. (1982): "Narcotic antagonistic
potency of bivalent ligands which contain l3-naltrexarnine. Evidence for bridging between
proximal recognition sites", J. Med. Chem., 25:847-849.
PORTOGHESE, P. S., RONSISVALLE, G., LARSON, D. L., YIM, C. B., SA YRE, L. M.
and TAKEMORI, A. E. (1982): "Opioid agonist and antagonist bivalent ligands as
receptor probes", Lije Sci., 31:1283-1286.
PORTOGHESE, P. S., LARSON, D. L., SAYRE, L. M., YIM, C. B., RONSISVALLE,
G., TAM, S. W. and TAKEMORI, A. E. (1986): "Opioid agonist and antagonist bivalent
ligands. The relationship between spacer lenght and selectivity at multiple opioid receptors",
J. Med. Chem., 29:1855-1861.
PORTOGHESE, P. S., RONSISV ALLE, G., LARSON, D. L. and TAKEMORI, A. E.
(1986): "Synthesis and opioid antagonist potencies of naltrexarnine bivalent ligands with
conformationally restricted spacers", J. Med. Chem., 29:1650-1653.
PORTOGHESE, P. S., LARSON, D. L., YIM, C. B., SA YRE, L. M., RONSISVALLE,
G., LIPKOWSKI, A. W., T AKEMORI, A. E., RICE, K. C. and T AM, S. W. (1985):
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