- 3-(1H-tetrazol-5-yl)-1,4,5,6-tetrahydro-cyclopentapyrazole (MK-0354): a partial agonist of the nicotinic acid receptor, G-protein coupled receptor 109a, with antilipolytic but no vasodilatory activity in mice.
3-(1H-tetrazol-5-yl)-1,4,5,6-tetrahydro-cyclopentapyrazole (MK-0354): a partial agonist of the nicotinic acid receptor, G-protein coupled receptor 109a, with antilipolytic but no vasodilatory activity in mice.
Journal of medicinal chemistry (2008-07-31)
Graeme Semple, Philip J Skinner, Tawfik Gharbaoui, Young-Jun Shin, Jae-Kyu Jung, Martin C Cherrier, Peter J Webb, Susan Y Tamura, P Douglas Boatman, Carleton R Sage, Thomas O Schrader, Ruoping Chen, Steven L Colletti, James R Tata, M Gerard Waters, Kang Cheng, Andrew K Taggart, Tian-Quan Cai, Ester Carballo-Jane, Dominic P Behan, Daniel T Connolly, Jeremy G Richman
PMID18665582
ZUSAMMENFASSUNG
The discovery and profiling of 3-(1H-tetrazol-5-yl)-1,4,5,6-tetrahydro-cyclopentapyrazole (5a, MK-0354), a partial agonist of GPR109a, is described. Compound 5a retained the plasma free fatty acid lowering effects in mice associated with GPR109a agonism, but did not induce vasodilation at the maximum feasible dose. Moreover, preadministration of 5a blocked the flushing effect induced by nicotinic acid but not that induced by PGD2. This profile made 5a a suitable candidate for further study for the treatment of dyslipidemia.
MATERIALIEN
Produktnummer
Marke
Produktbeschreibung
Sigma-Aldrich
Nicotinsäure, BioReagent, suitable for cell culture, suitable for insect cell culture, suitable for plant cell culture, ≥98%