Discovery of 1-[3-(4-Bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxyphenyl]-3-(2, 4-difluorophenyl)urea (Nelotanserin) and Related 5-Hydroxytryptamine 2A Inverse Agonists for the Treatment of Insomnia

Journal of Medicinal Chemistry

Volumn 53, Issue 5, 2010, Pages 1923-1936

  Teegarden, Bradley R ^a   Li, Hongmei ^a   Jayakumar, Honnappa ^a   Strah Pleynet, Sonja ^a   Dosa, Peter I ^a   Selaya, Susan D ^a   Kato, Naomi ^a   Elwell, Katie H ^a   Davidson, Jarrod ^a   Cheng, Karen ^a   Saldana, Hazel ^a   Frazer, John M ^a   Whelan, Kevin ^a   Foster, Jonathan ^a   Espitia, Stephan ^a   Webb, Robert R ^a   Beeley, Nigel R A ^a   Thomsen, William ^a   Morairty, Stephen R ^b   Kilduff, Thomas S ^b   Al Shamma, Hussien A ^a   more..

^a ARENA PHARMACEUTICALS   (United States)

^b SRI INTERNATIONAL   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 [3 (4 BROMO 2 METHYL 2H PYRAZOL 3 YL) 4 METHOXYPHENYL] 3 (2,4 DIFLUOROPHENYL)UREA; 5 HYDROXYTRYPTAMINE 2A; APD 125; DIPHENYL ETHER; PHENYLPYRAZOLEUREA DERIVATIVE; PYRAZOLE; SEROTONIN AGONIST; SEROTONIN DERIVATIVE; UNCLASSIFIED DRUG; UREA DERIVATIVE;

ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; AROUSAL; ARTICLE; CONTROLLED STUDY; DRUG ACTIVITY; DRUG BINDING; DRUG HALF LIFE; DRUG STRUCTURE; INSOMNIA; MALE; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; NONREM SLEEP; RAT; SLEEP; STRUCTURE ACTIVITY RELATION; SUZUKI REACTION; TIME TO MAXIMUM PLASMA CONCENTRATION;

ANIMALS; BINDING, COMPETITIVE; INHIBITORY CONCENTRATION 50; MALE; PHENYLUREA COMPOUNDS; PYRAZOLES; RATS; RATS, WISTAR; RECEPTOR, SEROTONIN, 5-HT2A; RECEPTOR, SEROTONIN, 5-HT2C; SEROTONIN; SLEEP; SLEEP INITIATION AND MAINTENANCE DISORDERS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 77949420045     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm9007328     Document Type: Article

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