Discovery of novel Tricyclic full agonists for the G-protein-coupled niacin receptor 109A with minimized flushing in rats

Journal of Medicinal Chemistry

Volumn 52, Issue 8, 2009, Pages 2587-2602

  Shen, Hong C ^a   Ding, F X ^a   Deng, Qiaolin ^a   Wilsie, Larissa C ^a   Krsmanovic, Mihajlo L ^a   Taggart, Andrew K ^a   Carballo Jane, Ester ^a   Ren, Ning ^a   Cai, T Q ^a   Wu, T J ^a   Wu, Kenneth K ^a   Cheng, Kang ^a   Chen, Qing ^a   Wolff, Michael S ^a   Tong, Xinchun ^a   Holt, Tom G ^a   Waters, M Gerard ^a   Hammond, Milton L ^a   Tata, James R ^a   Colletti, Steven L ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTHRANILIC ACID; CARBOXYLIC ACID DERIVATIVE; CYCLOALKENE; CYTOCHROME P450 2C8; CYTOCHROME P450 2C9; FATTY ACID; G PROTEIN COUPLED RECEPTOR; G PROTEIN COUPLED RECEPTOR 109A; NICOTINIC ACID; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; DISTRIBUTION VOLUME; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG HALF LIFE; DRUG POTENCY; ENZYME INHIBITION; HUMAN; HUMAN CELL; IN VITRO STUDY; MALE; MOUSE; NONHUMAN; RAT; RECEPTOR AFFINITY; STRUCTURE ACTIVITY RELATION; VASODILATATION;

ADIPOCYTES; ANIMALS; ANTHRANILIC ACIDS; CHO CELLS; CRICETINAE; CRICETULUS; CYCLOPARAFFINS; EAR; FLUSHING; HETEROCYCLIC COMPOUNDS, 3-RING; HUMANS; HYPOLIPIDEMIC AGENTS; LIPOLYSIS; MALE; MICE; NIACIN; RADIOLIGAND ASSAY; RATS; RECEPTORS, G-PROTEIN-COUPLED; RECEPTORS, NICOTINIC; STRUCTURE-ACTIVITY RELATIONSHIP; VASODILATION;

EID: 65249138654     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm900151e     Document Type: Article

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