ARTICLE;
BINDING AFFINITY;
DRUG ANTAGONISM;
DRUG IDENTIFICATION;
DRUG POTENCY;
DRUG RECEPTOR BINDING;
HUMAN;
HUMAN CELL;
IN VITRO STUDY;
MOLECULAR MODEL;
PHARMACOPHORE;
RECEPTOR BLOCKING;
STRUCTURE ACTIVITY RELATION;
Ellis, G. P., Luscombe, D. K., Oxford, A. W., Eds.; Elsevier Science, Amsterdam
Schmidhammer, H. Opioid receptor antagonists. Progress in Medicinal Chemistry; Ellis, G. P., Luscombe, D. K., Oxford, A. W., Eds.; Elsevier Science, Amsterdam, 1998; Vol. 35, pp 83-132.
Methcinnamox is a potent, long-lasting and selective antagonist of morphine-mediated antinociception in the mouse: Comparison with clocinnamox, β-FNA and β-chlornaltrexamine
Broadbear, J. H.; Sumpter, T. L.; Burke, T. F.; Husbands, S. M.; Lewis, J. W.; Woods, J. H.; Traynor, J. R. Methcinnamox is a potent, long-lasting and selective antagonist of morphine-mediated antinociception in the mouse: Comparison with clocinnamox, β-FNA and β-chlornaltrexamine. J. Pharmacol. Exp. Ther. 2000, 294, 933-940.
Potent and selective indolomorphinan antagonists of the κ-opioid receptor
Stevens, W. C., Jr.; Jones, R. M.; Subramanian, G.; Metzger, T. G.; Ferguson, D. M.; Portoghese, P. S. Potent and selective indolomorphinan antagonists of the κ-opioid receptor. J. Med. Chem. 2000, 43, 2759-2769.
Binaltorphimine and nor-binaltorphimine, potent and selective kappa-opioid receptor antagonists
Portoghese, P. S.; Lipkowski, A. W.; Takemori, A. E. Binaltorphimine and nor-binaltorphimine, potent and selective kappa-opioid receptor antagonists. Life Sci. 1987, 40, 1287-1292.
5′-Guanidinonaltrindole, a highly selective and potent κ-opioid receptor antagonist
Jones, R. M.; Portoghese, P. S. 5′-Guanidinonaltrindole, a highly selective and potent κ-opioid receptor antagonist. Eur. J. Pharmacol. 2000, 396, 49-52.
Structure-activity relationships of trans-3,4-dimethyl-4-(3- hydroxyphenyl)piperidine antagonists for μ- and κ-opioid receptors
Zimmerman, D. M.; Leander, J. D.; Cantrell, B. E.; Reel, J. K.; Snoddy, J.; Mendelsohn, L. G.; Johnson, B. G.; Mitch, C. H. Structure-activity relationships of trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine antagonists for μ- and κ-opioid receptors. J. Med. Chem. 1993, 36, 2833-2841.
Investigation of the N-substituent conformation governing potency and μ receptor subtype-selectivity in (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)- piperidine opioid antagonists
Thomas, J. B.; Mascarella, S. W.; Rothman, R. B.; Partilla, J. S.; Xu, H.; McCullough, K. B.; Dersch, C. M.; Cantrell, B. E.; Zimmerman, D. M.; Carroll, F. I. Investigation of the N-substituent conformation governing potency and μ receptor subtype-selectivity in (+)-(3R,4R)-dimethyl-4-(3- hydroxyphenyl)-piperidine opioid antagonists. J. Med. Chem. 1998, 41, 1980-1990.
Identification of the first trans-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)- piperidine derivative to possess highly potent and selective κ receptor antagonist activity
Thomas, J. B.; Atkinson, R. N.; Rothman, R. B.; Fix, S. E.; Mascarella, S. W.; Vinson, N. A.; Xu, H.; Dersch, C. M.; Lu, Y.-F.; Cantrell, B. E.; Zimmerman, D. M.; Carroll, F. I. Identification of the first trans-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)-piperidine derivative to possess highly potent and selective κ receptor antagonist activity. J. Med. Chem. 2001, 44, 2687-2690.
Opioid ligands having delayed long-term antagonist activity: Potential pharmacotherapies for opioid abuse
Husbands, S. M.; Lewis, J. W. Opioid ligands having delayed long-term antagonist activity: Potential pharmacotherapies for opioid abuse. Mini-Rev. Med. Chem. 2003, 3, 137-144.
9-Oxobenzomorphans. I. General synthesis of dihydrobenz[e]indolines as key intermediates
Kavadias, G.; Velkof, S.; Belleau, B. 9-Oxobenzomorphans. I. General synthesis of dihydrobenz[e]indolines as key intermediates. Can. J. Chem. 1979, 57, 1852-1860. Kavadias, G.; Velkof, S.; Belleau, B. 9-Oxobenzomorphans. III. Synthesis of derivatives with various substituents at 2-, 2′-, and 5-positions. Can. J. Chem. 1979, 57, 1866-1869.
9-Oxobenzomorphans. III. Synthesis of derivatives with various substituents at 2-, 2′-, and 5-positions
Kavadias, G.; Velkof, S.; Belleau, B. 9-Oxobenzomorphans. I. General synthesis of dihydrobenz[e]indolines as key intermediates. Can. J. Chem. 1979, 57, 1852-1860. Kavadias, G.; Velkof, S.; Belleau, B. 9-Oxobenzomorphans. III. Synthesis of derivatives with various substituents at 2-, 2′-, and 5-positions. Can. J. Chem. 1979, 57, 1866-1869.
Substituted tetralins III: Synthesis and analgesic activities of some substituted 2-methyl and 2-benzyl-4,4-dimethyl-2-aminotetralins
Pai, S. V.; Parulkar, A. P.; Martin, A. R.; White, A. I. Substituted tetralins III: Synthesis and analgesic activities of some substituted 2-methyl and 2-benzyl-4,4-dimethyl-2-aminotetralins. J. Pharm. Sci. 1971, 60, 201-205.
Bridged aminotetralins as novel potent analgesic substances
Freed, M. E.; Potoski, J. R.; Freed, E. H.; Conklin, G. L. Bridged aminotetralins as novel potent analgesic substances. J. Med. Chem. 1973, 16, 595-599.
Freed, M. E.; Potoski, J. R.; Freed, E. H.; Conklin, G. L.; Bell, S. C. Analgesic agents. 3. New bridged aminotetralins. J. Med. Chem. 1976, 19, 476-480.
Standard binding and functional assays related to (NIDA) Medications Development Division testing for potential cocaine and narcotic treatment programs
Toll, L.; Berzetei-Gurske, I. P.; Polgar, W. E.; Brandt, S. R.; Adapa, I. D.; Rodriguez, L.; Schwartz, R. W.; Haggart, D.; O'Brien, A.; White, A.; Kennedy, J. M., Craymer, K.; Farrington, L.; Auh, J. S. Standard binding and functional assays related to (NIDA) Medications Development Division testing for potential cocaine and narcotic treatment programs. NIDA Res. Monogr. 1998, 178, 440-466.