New developments in opioid receptors ligands
Resumen
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-l position showed high affinity and selectivity for
K opioid receptor subpopulations. MPCB and CCB were selected as specific K agonists.
The affinity ofCCB 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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Citas
RAYNOR, K., KONG, H., CHEN, Y., YASUDA, K., YU, L., BELL, G. I. and REISlNE,
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):
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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Publicado
1995-09-20
Cómo citar
1.
RONSTSVALLE G, PREZZAVENTO O, PASQUTNUCCI L, MARRAZZO A. New developments in opioid receptors ligands. Ars Pharm [Internet]. 20 de septiembre de 1995 [citado 5 de mayo de 2024];36(3):433-4. Disponible en: https://revistaseug.ugr.es/index.php/ars/article/view/21885
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