Discovery of pyrazolopyrimidines as the first class of allosteric agonists for the high affinity nicotinic acid receptor GPR109A.
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Shen HC, Taggart AK, Wilsie LC, Waters MG, Hammond ML, Tata JR, Colletti SL
Discovery of pyrazolopyrimidines as the first class of allosteric agonists for the high affinity nicotinic acid receptor GPR109A.
Bioorg Med Chem Lett. 2008 Sep 15;18(18):4948-51. doi: 10.1016/j.bmcl.2008.08.039. Epub 2008 Aug 14.
- PubMed ID
- 18752940 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Niacin Hydroxycarboxylic acid receptor 2 EC 50 (nM) 1000 N/A N/A Details Niacin Hydroxycarboxylic acid receptor 2 IC 50 (nM) 150 N/A N/A Details