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Items: 1 to 20 of 100

1.

Long-acting κ opioid antagonists nor-BNI, GNTI and JDTic: pharmacokinetics in mice and lipophilicity.

Munro TA, Berry LM, Van't Veer A, Béguin C, Carroll FI, Zhao Z, Carlezon WA Jr, Cohen BM.

BMC Pharmacol. 2012 May 29;12:5. doi: 10.1186/1471-2210-12-5.

2.

Selective κ opioid antagonists nor-BNI, GNTI and JDTic have low affinities for non-opioid receptors and transporters.

Munro TA, Huang XP, Inglese C, Perrone MG, Van't Veer A, Carroll FI, Béguin C, Carlezon WA Jr, Colabufo NA, Cohen BM, Roth BL.

PLoS One. 2013 Aug 14;8(8):e70701. doi: 10.1371/journal.pone.0070701. eCollection 2013.

3.

Physical presence of nor-binaltorphimine in mouse brain over 21 days after a single administration corresponds to its long-lasting antagonistic effect on κ-opioid receptors.

Patkar KA, Wu J, Ganno ML, Singh HD, Ross NC, Rasakham K, Toll L, McLaughlin JP.

J Pharmacol Exp Ther. 2013 Sep;346(3):545-54. doi: 10.1124/jpet.113.206086. Epub 2013 Jul 12.

4.

Pharmacokinetic evidence for the long-lasting effect of nor-binaltorphimine, a potent kappa opioid receptor antagonist, in mice.

Kishioka S, Kiguchi N, Kobayashi Y, Yamamoto C, Saika F, Wakida N, Ko MC, Woods JH.

Neurosci Lett. 2013 Sep 27;552:98-102. doi: 10.1016/j.neulet.2013.07.040. Epub 2013 Aug 7.

PMID:
23933210
5.

The kappa-opioid antagonist GNTI reduces U50,488-, DAMGO-, and deprivation-induced feeding, but not butorphanol- and neuropeptide Y-induced feeding in rats.

Jewett DC, Grace MK, Jones RM, Billington CJ, Portoghese PS, Levine AS.

Brain Res. 2001 Aug 3;909(1-2):75-80.

PMID:
11478923
6.

Kappa opioid antagonist effects of the novel kappa antagonist 5'-guanidinonaltrindole (GNTI) in an assay of schedule-controlled behavior in rhesus monkeys.

Negus SS, Mello NK, Linsenmayer DC, Jones RM, Portoghese PS.

Psychopharmacology (Berl). 2002 Oct;163(3-4):412-9. Epub 2002 Mar 13.

PMID:
12373442
7.

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
8.

Characterization of BU09059: a novel potent selective κ-receptor antagonist.

Casal-Dominguez JJ, Furkert D, Ostovar M, Teintang L, Clark MJ, Traynor JR, Husbands SM, Bailey SJ.

ACS Chem Neurosci. 2014 Mar 19;5(3):177-84. doi: 10.1021/cn4001507. Epub 2014 Jan 28.

9.

Pharmacological properties of JDTic: a novel kappa-opioid receptor antagonist.

Carroll I, Thomas JB, Dykstra LA, Granger AL, Allen RM, Howard JL, Pollard GT, Aceto MD, Harris LS.

Eur J Pharmacol. 2004 Oct 6;501(1-3):111-9.

PMID:
15464069
10.

Design, synthesis, and pharmacological evaluation of JDTic analogs to examine the significance of the 3- and 4-methyl substituents.

Carroll FI, Gichinga MG, Kormos CM, Maitra R, Runyon SP, Thomas JB, Mascarella SW, Decker AM, Navarro HA.

Bioorg Med Chem. 2015 Oct 1;23(19):6379-88. doi: 10.1016/j.bmc.2015.08.025. Epub 2015 Aug 25.

11.

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
12.
13.

A Double-Blind, Placebo-Controlled Trial to Evaluate the Safety, Tolerability, and Pharmacokinetics of Single, Escalating Oral Doses of JDTic.

Buda JJ, Carroll FI, Kosten TR, Swearingen D, Walters BB.

Neuropsychopharmacology. 2015 Aug;40(9):2059-65. doi: 10.1038/npp.2015.27. Epub 2015 Jan 23.

14.

Structure of the human κ-opioid receptor in complex with JDTic.

Wu H, Wacker D, Mileni M, Katritch V, Han GW, Vardy E, Liu W, Thompson AA, Huang XP, Carroll FI, Mascarella SW, Westkaemper RB, Mosier PD, Roth BL, Cherezov V, Stevens RC.

Nature. 2012 Mar 21;485(7398):327-32. doi: 10.1038/nature10939.

15.

Kappa receptor bivalent ligands.

Peng X, Neumeyer JL.

Curr Top Med Chem. 2007;7(4):363-73. Review.

PMID:
17305578
16.

Discovery of the first small-molecule opioid pan antagonist with nanomolar affinity at mu, delta, kappa, and nociceptin opioid receptors.

Zaveri NT, Journigan VB, Polgar WE.

ACS Chem Neurosci. 2015 Apr 15;6(4):646-57. doi: 10.1021/cn500367b. Epub 2015 Feb 18.

17.

Nalfurafine prevents 5'-guanidinonaltrindole- and compound 48/80-induced spinal c-fos expression and attenuates 5'-guanidinonaltrindole-elicited scratching behavior in mice.

Inan S, Dun NJ, Cowan A.

Neuroscience. 2009 Sep 29;163(1):23-33. doi: 10.1016/j.neuroscience.2009.06.016. Epub 2009 Jun 10.

18.

The kappa opioid receptor antagonist JDTic attenuates alcohol seeking and withdrawal anxiety.

Schank JR, Goldstein AL, Rowe KE, King CE, Marusich JA, Wiley JL, Carroll FI, Thorsell A, Heilig M.

Addict Biol. 2012 May;17(3):634-47. doi: 10.1111/j.1369-1600.2012.00455.x.

19.

The dynamic relationship between mu and kappa opioid receptors in body temperature regulation.

Chen X, McClatchy DB, Geller EB, Tallarida RJ, Adler MW.

Life Sci. 2005 Dec 12;78(4):329-33. Epub 2005 Oct 28.

PMID:
16257420
20.

Intracisternal nor-binaltorphimine distinguishes central and peripheral kappa-opioid antinociception in rhesus monkeys.

Ko MC, Johnson MD, Butelman ER, Willmont KJ, Mosberg HI, Woods JH.

J Pharmacol Exp Ther. 1999 Dec;291(3):1113-20.

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