Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists

Journal of Medicinal Chemistry

Volumn 52, Issue 9, 2009, Pages 3039-3046

  Jiang, Jinlong ^a   Bunda, Jaime L ^a   Doss, Geoge A ^a   Chicchi, Gary G ^a   Kurtz, Marc M ^a   Tsao, Kwei Lan C ^a   Tong, Xinchun ^a   Zheng, Song ^a   Upthagrove, Alana ^a   Samuel, Koppara ^a   Tschirret Guth, Richard ^a   Kumar, Sanjeev ^a   Wheeldon, Alan ^b   Carlson, Emma J ^b   Hargreaves, Richard ^a   Burns, Donald ^a   Hamill, Terence ^a   Ryan, Christine ^a   Krause, Stephen M ^a   Eng, WaiSi ^a   DeVita, Robert J ^a   Mills, Sander G ^a   more..

^a MERCK RESEARCH LABORATORIES   (United States)

^b NEUROSCIENCE RESEARCH CENTRE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

3 [5 [1 [3,5 BIS(TRIFLUOROMETHYL)PHENYL]ETHOXY] 4 (4 FLUOROPHENYL)OCTAHYDRO 2H ISOINDOL 2 YL]CYCLOPENT 2 EN 1 ONE; APREPITANT; NEUROKININ 1 RECEPTOR ANTAGONIST; UNCLASSIFIED DRUG;

ALKYLATION; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; AREA UNDER THE CURVE; ARTICLE; CHEMOTHERAPY INDUCED EMESIS; CONTROLLED STUDY; DIELS ALDER REACTION; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG HALF LIFE; DRUG PENETRATION; DRUG RECEPTOR BINDING; DRUG STRUCTURE; DRUG SYNTHESIS; NONHUMAN; POSITRON EMISSION TOMOGRAPHY; POSTOPERATIVE VOMITING; RHESUS MONKEY;

ADMINISTRATION, ORAL; ANIMALS; BRAIN; CHO CELLS; CRICETINAE; CRICETULUS; DRUG INTERACTIONS; ENZYME INHIBITORS; HUMANS; INHIBITORY CONCENTRATION 50; ISOINDOLES; MACACA MULATTA; MORPHOLINES; RECEPTORS, NEUROKININ-1; STEREOISOMERISM;

EID: 65649132794     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm8016514     Document Type: Article

References (15)

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