Thomas JB - Search Results

1

Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor.

Thomas JB, Zhang L, Navarro HA, Carroll FI. Thomas JB, et al. J Med Chem. 2006 Sep 7;49(18):5597-609. doi: 10.1021/jm060459p. J Med Chem. 2006. PMID: 16942033

2

Discovery of an opioid kappa receptor selective pure antagonist from a library of N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphans.

Thomas JB, Atkinson RN, Namdev N, Rothman RB, Gigstad KM, Fix SE, Mascarella SW, Burgess JP, Vinson NA, Xu H, Dersch CM, Cantrell BE, Zimmerman DM, Carroll FI. Thomas JB, et al. J Med Chem. 2002 Aug 1;45(16):3524-30. doi: 10.1021/jm020084h. J Med Chem. 2002. PMID: 12139463

3

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

4

Discovery of the first N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphan to possess highly potent and selective opioid delta receptor antagonist activity.

Carroll FI, Zhang L, Mascarella SW, Navarro HA, Rothman RB, Cantrell BE, Zimmerman DM, Thomas JB. Carroll FI, et al. Among authors: thomas jb. J Med Chem. 2004 Jan 15;47(2):281-4. doi: 10.1021/jm030419a. J Med Chem. 2004. PMID: 14711299

5

Importance of phenolic address groups in opioid kappa receptor selective antagonists.

Thomas JB, Fix SE, Rothman RB, Mascarella SW, Dersch CM, Cantrell BE, Zimmerman DM, Carroll FI. Thomas JB, et al. J Med Chem. 2004 Feb 12;47(4):1070-3. doi: 10.1021/jm030467v. J Med Chem. 2004. PMID: 14761209

6

N-substituted cis-4a-(3-hydroxyphenyl)-8a-methyloctahydroisoquinolines are opioid receptor pure antagonists.

Carroll FI, Chaudhari S, Thomas JB, Mascarella SW, Gigstad KM, Deschamps J, Navarro HA. Carroll FI, et al. Among authors: thomas jb. J Med Chem. 2005 Dec 29;48(26):8182-93. doi: 10.1021/jm058261c. J Med Chem. 2005. PMID: 16366600 Free PMC article.

7

N-substituted 4beta-methyl-5-(3-hydroxyphenyl)-7alpha-amidomorphans are potent, selective kappa opioid receptor antagonists.

Carroll FI, Melvin MS, Nuckols MC, Mascarella SW, Navarro HA, Thomas JB. Carroll FI, et al. Among authors: thomas jb. J Med Chem. 2006 Mar 9;49(5):1781-91. doi: 10.1021/jm058264p. J Med Chem. 2006. PMID: 16509593

8

A new synthesis of the ORL-1 antagonist 1-[(3R,4R)-1-cyclooctylmethyl-3-hydroxymethyl-4-piperidinyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one (J-113397) and activity in a calcium mobilization assay.

Smith ED, Ariane Vinson N, Zhong D, Berrang BD, Catanzaro JL, Thomas JB, Navarro HA, Gilmour BP, Deschamps J, Carroll FI. Smith ED, et al. Among authors: thomas jb. Bioorg Med Chem. 2008 Jan 15;16(2):822-9. doi: 10.1016/j.bmc.2007.10.023. Epub 2007 Oct 13. Bioorg Med Chem. 2008. PMID: 17976996 Free PMC article.

9

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

10

The identification of nonpeptide neurotensin receptor partial agonists from the potent antagonist SR48692 using a calcium mobilization assay.

Thomas JB, Navarro H, Warner KR, Gilmour B. Thomas JB, et al. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1438-41. doi: 10.1016/j.bmcl.2009.01.024. Epub 2009 Jan 15. Bioorg Med Chem Lett. 2009. PMID: 19195889 Free PMC article.

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