Abstract
A series of 3-nitro-4-substituted-aminobenzoic acids were prepared and found to act as potent and highly selective agonists of the orphan human GPCR GPR109b, a low affinity receptor for niacin. No activity was observed at the closely homologous high affinity niacin receptor, GPR109a. A second series, comprising 6-amino-substituted nicotinic acids was, also prepared and several analogues showed comparable activity to the nitroaryl series.
MeSH terms
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Animals
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Benzoates / agonists
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Benzoates / chemistry*
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Benzoates / metabolism
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CHO Cells
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Cricetinae
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Cricetulus
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Humans
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Niacin / metabolism
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Nicotinic Acids / agonists
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Nicotinic Acids / chemistry*
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Nicotinic Acids / metabolism
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Receptors, G-Protein-Coupled / agonists*
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Receptors, G-Protein-Coupled / metabolism
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Receptors, G-Protein-Coupled / physiology
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Receptors, Nicotinic / metabolism
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Receptors, Nicotinic / physiology
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Structure-Activity Relationship
Substances
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Benzoates
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HCAR2 protein, human
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HCAR3 protein, human
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Nicotinic Acids
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Receptors, G-Protein-Coupled
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Receptors, Nicotinic
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Niacin