Discovery of pyrazolopyrimidines as the first class of allosteric agonists for the high affinity nicotinic acid receptor GPR109A
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- 作者：Hong C. Shen ; Andrew K.P. Taggart ; Larissa C. Wilsie ; M. Gerard Waters ; Milton L. Hammond ; James R. Tata ; Steven L. Colletti
- 关键词：Pyrazolopyrimidines ; Allosteric agonists ; Nicotinic acid receptor ; GPR109A
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2008
- 出版时间：15 September 2008
- 年：2008
- 卷：18
- 期：18
- 页码：4948-4951
- 全文大小：201 K
文摘
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.