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Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity.
Thomas JB, Atkinson RN, Rothman RB, Fix SE, Mascarella SW, Vinson NA, Xu H, Dersch CM, Lu Y, Cantrell BE, Zimmerman DM, Carroll FI. Thomas JB, et al. J Med Chem. 2001 Aug 16;44(17):2687-90. doi: 10.1021/jm015521r. J Med Chem. 2001. PMID: 11495579
Effect of N-alkyl and N-alkenyl substituents in noroxymorphindole, 17-substituted-6,7-dehydro-4,5alpha-epoxy-3,14-dihydroxy-6,7:2',3'-indolomorphinans, on opioid receptor affinity, selectivity, and efficacy.
McLamore S, Ullrich T, Rothman RB, Xu H, Dersch C, Coop A, Davis P, Porreca F, Jacobson AE, Rice KC. McLamore S, et al. J Med Chem. 2001 Apr 26;44(9):1471-4. doi: 10.1021/jm000511w. J Med Chem. 2001. PMID: 11311071
Factors influencing agonist potency and selectivity for the opioid delta receptor are revealed in structure-activity relationship studies of the 4-[(N-substituted-4-piperidinyl)arylamino]-N,N-diethylbenzamides.
Thomas JB, Herault XM, Rothman RB, Atkinson RN, Burgess JP, Mascarella SW, Dersch CM, Xu H, Flippen-Anderson JL, George CF, Carroll FI. Thomas JB, et al. J Med Chem. 2001 Mar 15;44(6):972-87. doi: 10.1021/jm000427g. J Med Chem. 2001. PMID: 11300879
Probes for narcotic receptor-mediated phenomena. 27. Synthesis and pharmacological evaluation of selective delta-opioid receptor agonists from 4-[(alphaR)-alpha-(2S,5R)-4-substituted-2, 5-dimethyl-1-piperazinyl-3-methoxybenzyl]-N,N-diethylbenzamides and their enantiomers.
Furness MS, Zhang X, Coop A, Jacobson AE, Rothman RB, Dersch CM, Xu H, Porreca F, Rice KC. Furness MS, et al. J Med Chem. 2000 Aug 10;43(16):3193-6. doi: 10.1021/jm0001222. J Med Chem. 2000. PMID: 10956228
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