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Shen, Hong C.; Szymonifka, Michael J.; Kharbanda, Divya; Deng, Qiaolin; Carballo-Jane, Ester; Wu, Kenneth K.; Wu, Tsuei-Ju; Cheng, Kang; Ren, Ning; Cai, Tian-Quan; Taggart, Andrew K.; Wang, Junying; Tong, Xinchun; Waters, M. Gerard; Hammond, Milton L.; Tata, James R.; Colletti, Steven L.
Bioorganic & medicinal chemistry letters, 12/2007, Letnik: 17, Številka: 24Journal Article
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 also demonstrated equal affinity to GPR109A as niacin. 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.
