5-N,N-Disubstituted 5-aminopyrazole-3-carboxylic acids are highly potent agonists of GPR109b |
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| Authors: | Philip J Skinner Peter J Webb Carleton R Sage Huong T Dang Cameron C Pride Ruoping Chen Susan Y Tamura Jeremy G Richman Daniel T Connolly Graeme Semple |
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| Affiliation: | 1. Medicinal Chemistry, Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, CA, 92121, USA;2. Discovery Biology, Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, CA, 92121, USA |
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| 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. |
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