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Bioorg Med Chem Lett. 2008 Sep 15;18(18):4948-51. doi: 10.1016/j.bmcl.2008.08.039. Epub 2008 Aug 14.

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

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065-0900, USA. hong_shen@merck.com

Abstract

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.

PMID:
18752940
DOI:
10.1016/j.bmcl.2008.08.039
[Indexed for MEDLINE]

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