Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 51, Issue 16, Pages 5101-5108Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm800258p
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The discovery and profiling of 3-(1H-tetrazol-5-yl)-1,4,5,6-tetrahydro-cyclopeiitapyrazole (5a, MK-0354), a partial agonist of GPR 109a, is described. Compound 5a retained the plasma free fatty acid lowering effects in mice associated with GPR109a agonism, but did not induce vasodilation at the maximum feasible dose. Moreover, preadministration of 5a blocked the flushing effect induced by nicotinic acid but not that induced by PGD(2). This profile made 5a a suitable candidate for further study for the treatment of dyslipidemia.
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