Abstract
5-Alkyl and aryl-pyrazole-tetrazoles have been identified as a new class of selective, small-molecule, agonists of the human G-protein-coupled receptor GPR109a, a high affinity receptor for the HDL-raising drug nicotinic acid.
MeSH terms
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Animals
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Humans
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Male
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Mice
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Mice, Inbred C57BL
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Mice, Knockout
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Nicotinic Agonists / chemistry
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Nicotinic Agonists / pharmacology
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Pyrazoles / chemistry*
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Pyrazoles / pharmacology
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Receptors, G-Protein-Coupled / agonists*
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Receptors, G-Protein-Coupled / deficiency
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Receptors, G-Protein-Coupled / physiology
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Receptors, Nicotinic / deficiency
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Receptors, Nicotinic / physiology
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Tetrazoles / chemistry*
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Tetrazoles / pharmacology
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Vasodilation / drug effects
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Vasodilation / physiology
Substances
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HCAR2 protein, human
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Nicotinic Agonists
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Pyrazoles
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Receptors, G-Protein-Coupled
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Receptors, Nicotinic
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Tetrazoles
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pyrazole