Pyrazole acids as niacin receptor agonists for the treatment of dyslipidemia.

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Schmidt D, Smenton A, Raghavan S, Carballo-Jane E, Lubell S, Ciecko T, Holt TG, Wolff M, Taggart A, Wilsie L, Krsmanovic M, Ren N, Blom D, Cheng K, McCann PE, Gerard Waters M, Tata J, Colletti S

Pyrazole acids as niacin receptor agonists for the treatment of dyslipidemia.

Bioorg Med Chem Lett. 2009 Aug 15;19(16):4768-72. doi: 10.1016/j.bmcl.2009.06.054. Epub 2009 Jun 17.

PubMed ID

19592242 [ View in PubMed

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Abstract

Niacin is an effective drug for raising HDL cholesterol and reducing coronary risks, but patients show low compliance with treatment due to severe facial flushing upon taking the drug. A series of bicyclic pyrazole carboxylic acids were synthesized and tested for their ability to activate the niacin receptor. One analog, 23, showed improved potency and lacked flushing at doses that effectively altered the lipid profile of rats.

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
Niacin	Hydroxycarboxylic acid receptor 2	IC 50 (nM)	140	N/A	N/A	Details