Potent tricyclic pyrazole tetrazole agonists of the nicotinic acid receptor (GPR109a).
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Boatman PD, Schrader TO, Kasem M, Johnson BR, Skinner PJ, Jung JK, Xu J, Cherrier MC, Webb PJ, Semple G, Sage CR, Knudsen J, Chen R, Taggart AK, Carballo-Jane E, Richman JG
Potent tricyclic pyrazole tetrazole agonists of the nicotinic acid receptor (GPR109a).
Bioorg Med Chem Lett. 2010 May 1;20(9):2797-800. doi: 10.1016/j.bmcl.2010.03.062. Epub 2010 Mar 20.
- PubMed ID
- 20363624 [ View in PubMed]
- Abstract
Tricyclic pyrazole tetrazoles which are potent partial agonists of the high affinity niacin receptor, GPR109a, have been discovered and optimized. One of these compounds has proven to be effective at lowering free fatty acids in vitro and in vivo.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Niacin Hydroxycarboxylic acid receptor 2 EC 50 (nM) 27 N/A N/A Details