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Bioorg Med Chem Lett. 2009 Aug 1;19(15):4207-9. doi: 10.1016/j.bmcl.2009.05.108. Epub 2009 May 30.

5-N,N-Disubstituted 5-aminopyrazole-3-carboxylic acids are highly potent agonists of GPR109b.

Author information

1
Medicinal Chemistry, Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, CA, 92121, USA. philip.j.skinner@gmail.com

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.

PMID:
19524438
DOI:
10.1016/j.bmcl.2009.05.108
[Indexed for MEDLINE]

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