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.
MeSH terms
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Animals
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Atherosclerosis / drug therapy
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CHO Cells
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Carboxylic Acids / chemical synthesis*
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Carboxylic Acids / pharmacology
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Chemistry, Pharmaceutical / methods
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Cricetinae
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Cricetulus
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Drug Design
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Dyslipidemias / drug therapy
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Humans
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Ligands
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Lipoproteins, HDL / chemistry
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Lipoproteins, LDL / chemistry
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Models, Chemical
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Niacin / chemistry
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Pyrazoles / pharmacology
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Receptors, G-Protein-Coupled / agonists*
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Receptors, G-Protein-Coupled / metabolism
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Receptors, Nicotinic
Substances
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Carboxylic Acids
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HCAR3 protein, human
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Ligands
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Lipoproteins, HDL
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Lipoproteins, LDL
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Pyrazoles
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Receptors, G-Protein-Coupled
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Receptors, Nicotinic
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Niacin