5-N,N-Disubstituted 5-aminopyrazole-3-carboxylic acids are highly potent agonists of GPR109b.
Article Details
- CitationCopy to clipboard
Skinner PJ, Webb PJ, Sage CR, Dang TH, Pride CC, Chen R, Tamura SY, Richman JG, Connolly DT, Semple G
5-N,N-Disubstituted 5-aminopyrazole-3-carboxylic acids are highly potent agonists of GPR109b.
Bioorg Med Chem Lett. 2009 Aug 1;19(15):4207-9. doi: 10.1016/j.bmcl.2009.05.108. Epub 2009 May 30.
- PubMed ID
- 19524438 [ View in PubMed]
- Abstract
A series of 5-N,N-disubstituted-5-aminopyrazole-3-carboxylic acids were prepared and found to act as highly potent and selective agonists of the G-Protein Coupled Receptor (GPCR) GPR109b, a low affinity receptor for niacin and some aromatic d-amino acids. Little activity was observed at the highly homologous higher affinity niacin receptor, GPR109a.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Niacin Hydroxycarboxylic acid receptor 2 EC 50 (nM) 26.92 N/A N/A Details