5-N,N-Disubstituted 5-aminopyrazole-3-carboxylic acids are highly potent agonists of GPR109b. Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] Journal article | | Title | 5-N,N-Disubstituted 5-aminopyrazole-3-carboxylic acids are highly potent agonists of GPR109b. | | Author(s) | Skinner PJ, Webb PJ, Sage CR, Dang HT, Pride CC, Chen R, Tamura SY, Richman JG, Connolly DT, Semple G | | Institution | Medicinal Chemistry, Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, CA, 92121, USA. | | Source | Bioorg Med Chem Lett 2009 May 30. | | 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. | | Language | ENG | | Pub Type(s) | JOURNAL ARTICLE
| | PubMed ID | 19524438 |
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