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Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist.
Thomas JB, Atkinson RN, Vinson NA, Catanzaro JL, Perretta CL, Fix SE, Mascarella SW, Rothman RB, Xu H, Dersch CM, Cantrell BE, Zimmerman DM, Carroll FI. Thomas JB, et al. J Med Chem. 2003 Jul 3;46(14):3127-37. doi: 10.1021/jm030094y. J Med Chem. 2003. PMID: 12825951
Synthesis and in vitro opioid receptor functional antagonism of analogues of the selective kappa opioid receptor antagonist (3R)-7-hydroxy-N-((1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic).
Cai TB, Zou Z, Thomas JB, Brieaddy L, Navarro HA, Carroll FI. Cai TB, et al. Among authors: thomas jb. J Med Chem. 2008 Mar 27;51(6):1849-60. doi: 10.1021/jm701344b. Epub 2008 Feb 29. J Med Chem. 2008. PMID: 18307295
Synthesis and in vitro opioid receptor functional antagonism of methyl-substituted analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl]-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic).
Cueva JP, Cai TB, Mascarella SW, Thomas JB, Navarro HA, Carroll FI. Cueva JP, et al. Among authors: thomas jb. J Med Chem. 2009 Dec 10;52(23):7463-72. doi: 10.1021/jm900756t. J Med Chem. 2009. PMID: 19954245 Free PMC article.
332 results