Discovery of orally bioavailable and novel urea agonists of the high affinity niacin receptor GPR109A.

Article Details

Citation

Shen HC, Szymonifka MJ, Kharbanda D, Deng Q, Carballo-Jane E, Wu KK, Wu TJ, Cheng K, Ren N, Cai TQ, Taggart AK, Wang J, Tong X, Waters MG, Hammond ML, Tata JR, Colletti SL

Discovery of orally bioavailable and novel urea agonists of the high affinity niacin receptor GPR109A.

Bioorg Med Chem Lett. 2007 Dec 15;17(24):6723-8. Epub 2007 Oct 18.

PubMed ID
18029181 [ View in PubMed
]
Abstract

A urea class of high affinity niacin receptor agonists was discovered. Compound 1a displayed good PK, better in vivo efficacy in reducing FFA in mouse than niacin, and no vasodilation in a mouse model. Compound 1q demonstrated equal affinity to GPR109A as niacin.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
NiacinHydroxycarboxylic acid receptor 2EC 50 (nM)1000N/AN/ADetails
NiacinHydroxycarboxylic acid receptor 2IC 50 (nM)140N/AN/ADetails