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Publikationer i urvalet

22 träffar

Bibliografisk träff 2018-08-29

Potent and Selective Tetrahydroisoquinoline Kappa Opioid Receptor Antagonists of Lead Compound (3 R)- N-[1 R)-1-(Cyclohexylmethyl)-2-methylpropyl]-7-hydroxy-1,2,3,4-tetrahydroisoquinoline-3-carboxamide (CDTic).

Kormos CM, Ondachi PW, Runyon SP, Thomas JB, Mascarella SW, Decker AM, Navarro HA, Fennell TR, Snyder RW, Carroll FI.

J Med Chem · research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.8b00674

Bibliografisk träff 2018-08-29

Potent and Selective Tetrahydroisoquinoline Kappa Opioid Receptor Antagonists of Lead Compound (3 R)-7-Hydroxy- N-[(1 S)-2-methyl-1-(piperidin-1-ylmethyl)propyl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamide (PDTic).

Ondachi PW, Kormos CM, Runyon SP, Thomas JB, Mascarella SW, Decker AM, Navarro HA, Fennell TR, Snyder RW, Carroll FI.

J Med Chem · research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.8b00673

Bibliografisk träff 2017-10-10

Selective kappa opioid antagonists for treatment of addiction, are we there yet?

Helal MA, Habib ES, Chittiboyina AG.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2017.10.012

Bibliografisk träff 2017-05-25

Simple Tetrahydroisoquinolines Are Potent and Selective Kappa Opioid Receptor Antagonists.

Kormos CM, Ondachi PW, Runyon SP, Thomas JB, Mascarella SW, Decker AM, Navarro HA, Carroll FI.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/acsmedchemlett.7b00115

Bibliografisk träff 2017-03-13

In silico design of novel probes for the atypical opioid receptor MRGPRX2.

Lansu K, Karpiak J, Liu J, Huang XP, McCorvy JD, Kroeze WK, Che T, Nagase H, Carroll FI, Jin J, Shoichet BK, Roth BL.

Nat Chem Biol · research-article; journal article · DOI 10.1038/nchembio.2334

Bibliografisk träff 2016-06-15

Design, synthesis, and pharmacological evaluation of JDTic analogs to examine the significance of replacement of the 3-hydroxyphenyl group with pyridine or thiophene bioisosteres.

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

Bioorg Med Chem · research-article; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmc.2016.06.029

Bibliografisk träff 2015-08-25

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 · research-article; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmc.2015.08.025

Bibliografisk träff 2014-12-11

Novel fluoroalkyl derivatives of selective kappa opioid receptor antagonist JDTic: Design, synthesis, pharmacology and molecular modeling studies.

Schmitt S, Colloc'h N, Perrio C.

Eur J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.ejmech.2014.12.016

Bibliografisk träff 2014-03-24

Antagonists of the kappa opioid receptor.

Urbano M, Guerrero M, Rosen H, Roberts E.

Bioorg Med Chem Lett · review; journal article · DOI 10.1016/j.bmcl.2014.03.040

Bibliografisk träff 2013-05-16

Discovery of N-{4-[(3-hydroxyphenyl)-3-methylpiperazin-1-yl]methyl-2-methylpropyl}-4-phenoxybenzamide analogues as selective kappa opioid receptor antagonists.

Kormos CM, Jin C, Cueva JP, Runyon SP, Thomas JB, Brieaddy LE, Mascarella SW, Navarro HA, Gilmour BP, Carroll FI.

J Med Chem · research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/jm400275h

Bibliografisk träff 2013-02-14

Development of κ opioid receptor antagonists.

Carroll FI, Carlezon WA.

J Med Chem · research-article; review; journal article; research support, n.i.h., extramural · DOI 10.1021/jm301783x

Bibliografisk träff 2011-10-26

Discovery of aminobenzyloxyarylamides as κ opioid receptor selective antagonists: application to preclinical development of a κ opioid receptor antagonist receptor occupancy tracer.

Mitch CH, Quimby SJ, Diaz N, Pedregal C, de la Torre MG, Jimenez A, Shi Q, Canada EJ, Kahl SD, Statnick MA, McKinzie DL, Benesh DR, Rash KS, Barth VN.

J Med Chem · journal article · DOI 10.1021/jm200789r

Bibliografisk träff 2010-07-01

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). Synthesis and in vitro and in vivo opioid receptor antagonist activity.

Runyon SP, Brieaddy LE, Mascarella SW, Thomas JB, Navarro HA, Howard JL, Pollard GT, Carroll FI.

J Med Chem · research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/jm1004978

Bibliografisk träff 2009-12-01

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.

J Med Chem · research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/jm900756t

Bibliografisk träff 2008-02-29

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.

J Med Chem · journal article; research support, n.i.h., extramural · DOI 10.1021/jm701344b

Bibliografisk träff 2007-08-16

Long-acting kappa opioid antagonists disrupt receptor signaling and produce noncompetitive effects by activating c-Jun N-terminal kinase.

Bruchas MR, Yang T, Schreiber S, Defino M, Kwan SC, Li S, Chavkin C.

J Biol Chem · research-article; journal article; research support, n.i.h., extramural · DOI 10.1074/jbc.m705540200

Bibliografisk träff 2007-08-09

Flavonoids as opioid receptor ligands: identification and preliminary structure-activity relationships.

Katavic PL, Lamb K, Navarro H, Prisinzano TE.

J Nat Prod · research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/np070194x

Bibliografisk träff 2006-03-01

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.

J Med Chem · journal article; research support, n.i.h., extramural · DOI 10.1021/jm058264p

Bibliografisk träff 2005-12-01

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 · research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/jm058261c

Bibliografisk träff 2004-02-01

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 · research support, u.s. gov't, p.h.s.; journal article · DOI 10.1021/jm030467v

Bibliografisk träff 2003-07-01

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 · research support, u.s. gov't, p.h.s.; journal article · DOI 10.1021/jm030094y

Bibliografisk träff 2003-05-01

2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy.

Carroll FI.

J Med Chem · research support, u.s. gov't, p.h.s.; address; review · DOI 10.1021/jm030092d