Discovery of 1-(3-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}phenyl) -2-imidazolidinone (GSK163090), a potent, selective, and orally active 5-HT 1A/B/D receptor antagonist

Journal of Medicinal Chemistry

Volumn 53, Issue 23, 2010, Pages 8228-8240

  Leslie, Colin P ^a   Biagetti, Matteo ^a   Bison, Silvia ^a   Bromidge, Steven M ^b   Di Fabio, Romano ^a   Donati, Daniele ^a,c   Falchi, Alessandro ^a,d   Garnier, Martine J ^a   Jaxa Chamiec, Albert ^a,e   Manchee, Gary ^a,f   Merlo, Giancarlo ^a   Pizzi, Domenica A ^a   Stasi, Luigi P ^a,g   Tibasco, Jessica ^a   Vong, Antonio ^b   Ward, Simon E ^b   Zonzini, Laura ^a  

^a GSK   (Italy)

^b GLAXOSMITHKLINE   (United Kingdom)

^c NERVIANO MEDICAL SCIENCES   (Italy)

^d CHIESI FARMACEUTICI S P A   (Italy)

^e IMPERIAL COLLEGE LONDON   (United Kingdom)

^f Pharmidex   (United Kingdom)

^g Rotta Research Laboratorium   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

1 [3 [2 [4 (2 METHYL 5 QUINOLINYL) 1 PIPERAZINYL]ETHYL]PHENYL] 2 IMIDAZOLIDINONE; ANTIDEPRESSANT AGENT; AUTORECEPTOR; GSK 163090; SEROTONIN 1A ANTAGONIST; SEROTONIN TRANSPORTER; SEROTONIN UPTAKE INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; BINDING AFFINITY; CONTROLLED STUDY; DRUG ACTIVITY; DRUG BINDING; HUMAN; HUMAN CELL; IN VIVO STUDY; MALE; NONHUMAN; RAT;

ADMINISTRATION, ORAL; ANIMALS; CHO CELLS; CHROMATOGRAPHY, LIQUID; CRICETULUS; DRUG DISCOVERY; HUMANS; IMIDAZOLES; MAGNETIC RESONANCE SPECTROSCOPY; MALE; QUINOLINES; RATS, SPRAGUE-DAWLEY; RECEPTORS, SEROTONIN; SEROTONIN ANTAGONISTS; TANDEM MASS SPECTROMETRY;

EID: 78649805179     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm100714c     Document Type: Article

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