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Results: 1 to 20 of 118

1.

Novel trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as mu opioid receptor antagonists with improved opioid receptor selectivity profiles.

Le Bourdonnec B, Barker WM, Belanger S, Wiant DD, Conway-James NC, Cassel JA, O'Neill TJ, Little PJ, DeHaven RN, DeHaven-Hudkins DL, Dolle RE.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):2006-12. doi: 10.1016/j.bmcl.2008.01.106. Epub 2008 Feb 2.

PMID:
18313920
[PubMed - indexed for MEDLINE]
2.

Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists.

Thomas JB, Mascarella SW, Rothman RB, Partilla JS, Xu H, McCullough KB, Dersch CM, Cantrell BE, Zimmerman DM, Carroll FI.

J Med Chem. 1998 May 21;41(11):1980-90.

PMID:
9599247
[PubMed - indexed for MEDLINE]
3.

N-Substituted 9beta-methyl-5-(3-hydroxyphenyl)morphans are opioid receptor pure antagonists.

Thomas JB, Zheng X, Mascarella SW, Rothman RB, Dersch CM, Partilla JS, Flippen-Anderson JL, George CF, Cantrell BE, Zimmerman DM, Carroll FI.

J Med Chem. 1998 Oct 8;41(21):4143-9.

PMID:
9767649
[PubMed - indexed for MEDLINE]
4.

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.

J Med Chem. 2001 Aug 16;44(17):2687-90.

PMID:
11495579
[PubMed - indexed for MEDLINE]
5.

Structure-activity relationships of trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine antagonists for mu- and kappa-opioid receptors.

Zimmerman DM, Leander JD, Cantrell BE, Reel JK, Snoddy J, Mendelsohn LG, Johnson BG, Mitch CH.

J Med Chem. 1993 Oct 1;36(20):2833-41.

PMID:
8410998
[PubMed - indexed for MEDLINE]
6.

Elucidation of the bioactive conformation of the N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine class of mu-opioid receptor antagonists.

Le Bourdonnec B, Goodman AJ, Michaut M, Ye HF, Graczyk TM, Belanger S, Herbertz T, Yap GP, DeHaven RN, Dolle RE.

J Med Chem. 2006 Dec 14;49(25):7278-89.

PMID:
17149858
[PubMed - indexed for MEDLINE]
7.

Biaryl piperidines as potent and selective delta opioid receptor ligands.

Liras S, McHardy SF, Allen MP, Segelstein BE, Heck SD, Bryce DK, Schmidt AW, Vanase-Frawley M, Callegari E, McLean S.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):503-7. doi: 10.1016/j.bmcl.2009.11.113. Epub 2009 Nov 26.

PMID:
20015649
[PubMed - indexed for MEDLINE]
8.

Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine.

Thomas JB, Fall MJ, Cooper JB, Rothman RB, Mascarella SW, Xu H, Partilla JS, Dersch CM, McCullough KB, Cantrell BE, Zimmerman DM, Carroll FI.

J Med Chem. 1998 Dec 17;41(26):5188-97.

PMID:
9857089
[PubMed - indexed for MEDLINE]
9.

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.

J Med Chem. 2004 Feb 12;47(4):1070-3.

PMID:
14761209
[PubMed - indexed for MEDLINE]
10.
11.

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.

J Med Chem. 2001 Apr 26;44(9):1471-4.

PMID:
11311071
[PubMed - indexed for MEDLINE]
12.

Probes for narcotic receptor mediated phenomena. 47. Novel C4a- and N-substituted-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-6-ols.

Iyer MR, Rothman RB, Dersch CM, Jacobson AE, Rice KC.

Bioorg Med Chem. 2013 Jun 1;21(11):3298-309. doi: 10.1016/j.bmc.2013.02.060. Epub 2013 Apr 3.

PMID:
23618710
[PubMed - indexed for MEDLINE]
Free PMC Article
13.

Synthesis and pharmacological evaluation of novel octahydro-1H-pyrido[1,2-a]pyrazine as mu-opioid receptor antagonists.

Le Bourdonnec B, Goodman AJ, Graczyk TM, Belanger S, Seida PR, DeHaven RN, Dolle RE.

J Med Chem. 2006 Dec 14;49(25):7290-306.

PMID:
17149859
[PubMed - indexed for MEDLINE]
14.

trans-3,4-dimethyl-4-(3-carboxamidophenyl)piperidines: a novel class of micro-selective opioid antagonists.

Le Bourdonnec B, Belanger S, Cassel JA, Stabley GJ, DeHaven RN, Dolle RE.

Bioorg Med Chem Lett. 2003 Dec 15;13(24):4459-62.

PMID:
14643346
[PubMed - indexed for MEDLINE]
15.

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.

J Med Chem. 2003 Jul 3;46(14):3127-37.

PMID:
12825951
[PubMed - indexed for MEDLINE]
16.

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.

J Med Chem. 2005 Dec 29;48(26):8182-93.

PMID:
16366600
[PubMed - indexed for MEDLINE]
Free PMC Article
17.

3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity.

Mitch CH, Leander JD, Mendelsohn LG, Shaw WN, Wong DT, Cantrell BE, Johnson BG, Reel JK, Snoddy JD, Takemori AE, et al.

J Med Chem. 1993 Oct 1;36(20):2842-50.

PMID:
8410999
[PubMed - indexed for MEDLINE]
18.

Comparison of [Dmt1]DALDA and DAMGO in binding and G protein activation at mu, delta, and kappa opioid receptors.

Zhao GM, Qian X, Schiller PW, Szeto HH.

J Pharmacol Exp Ther. 2003 Dec;307(3):947-54. Epub 2003 Oct 8.

PMID:
14534366
[PubMed - indexed for MEDLINE]
Free Article
19.

The in vitro pharmacological profile of TD-1211, a neutral opioid receptor antagonist.

Tsuruda PR, Vickery RG, Long DD, Armstrong SR, Beattie DT.

Naunyn Schmiedebergs Arch Pharmacol. 2013 Jun;386(6):479-91. doi: 10.1007/s00210-013-0850-7. Epub 2013 Apr 4.

PMID:
23549670
[PubMed - indexed for MEDLINE]
20.

In vivo rat brain opioid receptor binding of LY255582 assessed with a novel method using LC/MS/MS and the administration of three tracers simultaneously.

Need AB, McKinzie JH, Mitch CH, Statnick MA, Phebus LA.

Life Sci. 2007 Oct 13;81(17-18):1389-96. Epub 2007 Sep 19.

PMID:
17935738
[PubMed - indexed for MEDLINE]

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