Fluorinated pyrazole acids are agonists of the high affinity niacin receptor GPR109a.

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Skinner PJ, Cherrier MC, Webb PJ, Shin YJ, Gharbaoui T, Lindstrom A, Hong V, Tamura SY, Dang HT, Pride CC, Chen R, Richman JG, Connolly DT, Semple G

Fluorinated pyrazole acids are agonists of the high affinity niacin receptor GPR109a.

Bioorg Med Chem Lett. 2007 Oct 15;17(20):5620-3. Epub 2007 Aug 23.

PubMed ID

17804224 [ View in PubMed

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Abstract

A series of 5-alkyl pyrazole-3-carboxylic acids were prepared and found to act as potent and selective agonists of the human GPCR, GPR109a, the high affinity nicotinic acid receptor. No activity was observed at the highly homologous low affinity niacin receptor, GPR109b. A further series of 4-fluoro-5-alkyl pyrazole-3-carboxylic acids were shown to display similar potency. One example from the series was shown to have improved properties in vivo compared to niacin.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Niacin	Hydroxycarboxylic acid receptor 2	EC 50 (nM)	>1000	N/A	N/A	Details