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

DOI: 10.1021/jm800258p

Source and publish data:

Journal of Medicinal Chemistry p. 5101 - 5108 (2008)

Update date:2022-09-26

Topics:

Authors:

Semple, Graeme

Skinner, Philip J.

Gharbaoui, Tawfik

Shin, Young-Jun

Jung, Jae-Kyu

Cherrier, Martin C.

Webb, Peter J.

Tamura, Susan Y.

Boatman, P. Douglas

Sage, Carleton R.

Schrader, Thomas O.

Chen, Ruoping

Colletti, Steven L.

Tata, James R.

Waters, M. Gerard

Cheng, Kang

Taggart, Andrew K.

Cai, Tian-Quan

Carballo-Jane, Ester

Behan, Dominic P.

Connolly, Daniel T.

Richman, Jeremy G.

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Article abstract of DOI:10.1021/jm800258p

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,

Full text of DOI:10.1021/jm800258p

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