(1a R,5a R)1a,3,5,5a-tetrahydro-1 H-2,3-diaza-cyclopropa[a]pentalene-4- carboxylic acid (MK-1903): A potent GPR109a agonist that lowers free fatty acids in humans

Journal of Medicinal Chemistry

Volumn 55, Issue 8, 2012, Pages 3644-3666

  Boatman, P Douglas ^a   Lauring, Brett ^a   Schrader, Thomas O ^a   Kasem, Michelle ^a   Johnson, Benjamin R ^a   Skinner, Philip ^a   Jung, Jae Kyu ^a   Xu, Jerry ^a   Cherrier, Martin C ^a   Webb, Peter J ^a   Semple, Graeme ^a   Sage, Carleton R ^a   Knudsen, Jens ^a   Chen, Ruoping ^a   Luo, Wen Lin ^b   Caro, Luzelena ^b   Cote, Josee ^b   Lai, Eseng ^b   Wagner, John ^b   Taggart, Andrew K ^b   Carballo Jane, Ester ^b   Hammond, Milton ^b   Colletti, Steven L ^b   Tata, James R ^b   Connolly, Daniel T ^b   Waters, M Gerard ^b   Richman, Jeremy G ^a   more..

^a ARENA PHARMACEUTICALS   (United States)

^b MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1A,3,5,5A TETRAHYDRO 1H 2,3 DIAZA CYCLOPROPA[A]PENTALENE 4 CARBOXYLIC ACID; ANTILIPEMIC AGENT; CARBOXYLIC ACID DERIVATIVE; FATTY ACID; G PROTEIN COUPLED RECEPTOR; G PROTEIN COUPLED RECEPTOR 109A; MK 1903; NICOTINIC ACID; PLACEBO; UNCLASSIFIED DRUG; 1A,3,5,5A TETRAHYDRO 1H 2,3 DIAZACYCLOPROPA(A)PENTALENE 4 CARBOXYLIC ACID; 1A,3,5,5A-TETRAHYDRO-1H-2,3-DIAZACYCLOPROPA(A)PENTALENE-4-CARBOXYLIC ACID; HCAR2 PROTEIN, HUMAN; NICOTINIC RECEPTOR; PYRAZOLE DERIVATIVE; VASODILATOR AGENT;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DOUBLE BLIND PROCEDURE; DRUG DOSE ESCALATION; DRUG SAFETY; DRUG SCREENING; DRUG TOLERANCE; DYSLIPIDEMIA; FATTY ACID BLOOD LEVEL; FLUSHING; HUMAN; HUMAN CELL; HUMAN EXPERIMENT; LOW DRUG DOSE; MALE; NONHUMAN; NORMAL HUMAN; PHASE 1 CLINICAL TRIAL; PHASE 2 CLINICAL TRIAL; RANDOMIZED CONTROLLED TRIAL; RAT; SIDE EFFECT; SINGLE DRUG DOSE; ANIMAL; BLOOD; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; DRUG EFFECT; DRUG POTENTIATION; STEREOISOMERISM; SYNTHESIS;

ANIMALS; FATTY ACIDS, NONESTERIFIED; HUMANS; HYPOLIPIDEMIC AGENTS; MALE; NIACIN; PYRAZOLES; RATS; RECEPTORS, G-PROTEIN-COUPLED; RECEPTORS, NICOTINIC; STEREOISOMERISM; VASODILATOR AGENTS;

EID: 84860273364     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm2010964     Document Type: Article

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