Discovery and structure-activity relationship of 3-methoxy-N-(3-(1-methyl-1 H-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide (APD791): A highly selective 5-hydroxytryptamine2A receptor inverse agonist for the treatment of arterial thrombosis

Journal of Medicinal Chemistry

Volumn 53, Issue 11, 2010, Pages 4412-4421

  Xiong, Yifeng ^a   Teegarden, Bradley R ^a   Choi, Jin Sun Karoline ^a   Strah Pleynet, Sonja ^a   Decaire, Marc ^a   Jayakumar, Honnappa ^a   Dosa, Peter I ^a   Casper, Martin D ^a   Pham, Lan ^a   Feichtinger, Konrad ^a   Ullman, Brett ^a   Adams, John ^a   Yuskin, Diane ^a   Frazer, John ^a   Morgan, Michael ^a   Sadeque, Abu ^a   Chen, Weichao ^a   Webb, Robert R ^a   Connolly, Daniel T ^a   Semple, Graeme ^a   Al Shamma, Hussien ^a   more..

^a ARENA PHARMACEUTICALS   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 METHOXY N [3 (1 METHYL 1H PYRAZOL 5 YL) 4 (2 MORPHOLINOETHOXY)PHENYL]BENZAMIDE; 3 METHOXY N [3 (2 METHYL 2H PYRAZOL 3 YL) 4 (2 MORPHOLIN 4 YL ETHOXY)PHENYL]BENZAMIDE; 4 IODO 2,5 DIMETHOXYAMPHETAMINE; ANTICOAGULANT AGENT; APD 791; BENZAMIDE DERIVATIVE; IODINE 125; KETANSERIN; NELOTANSERIN; POTASSIUM CHANNEL HERG; PYRAZOLE DERIVATIVE; SARPOGRELATE; SEROTONIN; SEROTONIN 2A AGONIST; SEROTONIN 2A RECEPTOR; SEROTONIN 2B RECEPTOR; SEROTONIN 2C RECEPTOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTERY THROMBOSIS; ARTICLE; BINDING AFFINITY; BINDING COMPETITION; CONTINUOUS INFUSION; DOG; DRUG BIOAVAILABILITY; DRUG HALF LIFE; DRUG RECEPTOR BINDING; DRUG SAFETY; DRUG SELECTIVITY; DRUG SOLUBILITY; DRUG STRUCTURE; HUMAN; HUMAN CELL; ISOTOPE LABELING; LIVER MICROSOME; MONKEY; NONHUMAN; RAT; SPECIES COMPARISON; STRUCTURE ACTIVITY RELATION; THROMBOCYTE AGGREGATION; THROMBOCYTE AGGREGATION INHIBITION;

ANIMALS; ARTERIES; BENZAMIDES; DOGS; DRUG DISCOVERY; DRUG INVERSE AGONISM; FEMALE; HUMANS; INHIBITORY CONCENTRATION 50; MALE; MORPHOLINES; PLATELET AGGREGATION; PYRAZOLES; RATS; RECEPTOR, SEROTONIN, 5-HT2A; STRUCTURE-ACTIVITY RELATIONSHIP; SUBSTRATE SPECIFICITY; THROMBOSIS;

EID: 77953220832     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm100044a     Document Type: Article

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