Discovery of pyrazolopyrimidines as the first class of allosteric agonists for the high affinity nicotinic acid receptor GPR109A

…, MG Waters, ML Hammond, JR Tata, SL Colletti

文献索引：Shen, Hong C.; Taggart, Andrew K.P.; Wilsie, Larissa C.; Waters, M. Gerard; Hammond, Milton L.; Tata, James R.; Colletti, Steven L. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 18 p. 4948 - 4951

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被引用次数: 16

摘要

Pyrazolopyrimidines were discovered as the first class of allosteric agonists for the high affinity nicotinic acid receptor GPR109A. In addition to its intrinsic activity, compound 9n significantly enhances nicotinic acid binding to the receptor, thereby potentiating the functional efficacy of nicotinic acid.