3-Arylimino-2-indolones are potent and selective galanin GAL3 receptor antagonists

Journal of Medicinal Chemistry

Volumn 49, Issue 13, 2006, Pages 3757-3758

  Konkel, Michael J ^a   Lagu, Bharat ^a,c   Boteju, Lakmal W ^a,d   Jimenez, Hermogenes ^a   Noble, Stewart ^a,e   Walker, Mary W ^a   Chandrasena, Gamini ^a   Blackburn, Thomas P ^a,f   Nikam, Sham S ^b   Wright, Jon L ^b,g   Kornberg, Brian E ^b   Gregory, Tracy ^b   Pugsley, Thomas A ^b   Akunne, Hyacinth ^b   Zoski, Kim ^b   Wise, Lawrence D ^b  

^a LUNDBECK RESEARCH USA   (United States)

^b PFIZER INC   (United States)

^c JOHNSON AND JOHNSON   (United States)

^d Lexicon Pharmaceutical Corporation   (United States)

^e Kalypsys Inc   (United States)

^f Helicon Therapeutics Inc   (United States)

^g CELGENE CORPORATION   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1,3 DIHYDRO 1 PHENYL 3 [[3 (TRIFLUOROMETHYL)PHENYL]IMINO] 2H INDOL 2 ONE; GALANIN RECEPTOR 3; GALANIN RECEPTOR 3 BLOCKING AGENT; INDOLE DERIVATIVE; RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; DRUG EFFECT; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; NONHUMAN; PROTON NUCLEAR MAGNETIC RESONANCE; RAT; RECEPTOR AFFINITY; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS; THIN LAYER CHROMATOGRAPHY;

ANIMALS; BINDING, COMPETITIVE; BRAIN; CERCOPITHECUS AETHIOPS; COS CELLS; CYCLIC AMP; HUMANS; IMINES; INDOLES; LIGANDS; RADIOLIGAND ASSAY; RATS; RECEPTOR, GALANIN, TYPE 1; RECEPTOR, GALANIN, TYPE 2; RECEPTOR, GALANIN, TYPE 3; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 33745660988     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm060001n     Document Type: Article

References (19)

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17. i determination was done in duplicate.
18. b = 29 nM (n = 4).
19. 4 agonist or antagonist activity at concentrations up to 10 μM.