Synthesis and in vivo evaluation of phenethylpiperazine amides: Selective 5-hydroxytryptamine2A receptor antagonists for the treatment of insomnia

Journal of Medicinal Chemistry

Volumn 53, Issue 15, 2010, Pages 5696-5706

  Xiong, Yifeng ^a   Ullman, Brett ^a   Choi, Jin Sun Karoline ^a   Cherrier, Martin ^a   Strah Pleynet, Sonja ^a   Decaire, Marc ^a   Dosa, Peter I ^a   Feichtinger, Konrad ^a   Teegarden, Bradley R ^a   Frazer, John M ^a   Yoon, Woo H ^a   Shan, Yun ^a   Whelan, Kevin ^a   Hauser, Erin K ^a   Grottick, Andrew J ^a   Semple, Graeme ^a   Al Shamma, Hussien ^a  

^a ARENA PHARMACEUTICALS   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 [4 (4 BROMO 1 METHYL 1H PYRAZOLE 3 CARBONYL)PIPERAZIN 1 YL] 1 (4 FLUOROPHENYL)ETHANONE; 2 [4 (4 CHLORO 1 METHYL 1H PYRAZOLE 3 CARBONYL)PIPERAZIN 1 YL] 1 (4 FLUOROPHENYL)ETHANONE; NELOTANSERIN; PIPERAZINE DERIVATIVE; PRUVANSERIN; SEROTONIN 2A ANTAGONIST; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; DRUG INDICATION; DRUG METABOLISM; DRUG SELECTIVITY; DRUG STABILITY; DRUG SYNTHESIS; INSOMNIA; MALE; NONHUMAN; RAT; RECEPTOR AFFINITY; RECEPTOR BLOCKING; REM SLEEP;

ADMINISTRATION, ORAL; AMIDES; ANIMALS; BIOLOGICAL AVAILABILITY; BLOOD PROTEINS; BRAIN; DOGS; DRUG INVERSE AGONISM; HAPLORHINI; HUMANS; MALE; MICROSOMES, LIVER; PIPERAZINES; PROTEIN BINDING; PYRAZOLES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTOR, SEROTONIN, 5-HT2A; SLEEP; SLEEP INITIATION AND MAINTENANCE DISORDERS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 77955407564     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm100479q     Document Type: Article

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