Title of article
Fluorinated pyrazole acids are agonists of the high affinity niacin receptor GPR109a
Author/Authors
Philip J. Skinner، نويسنده , , Martin C. Cherrier، نويسنده , , Peter J. Webb، نويسنده , , Young-Jun Shin، نويسنده , , Tawfik Gharbaoui، نويسنده , , Andrew Lindstrom، نويسنده , , Vu Hong Thang، نويسنده , , Susan Y. Tamura، نويسنده , , Huong T. Dang، نويسنده , , Cameron C. Pride، نويسنده , , Ruoping Chen، نويسنده , , Jeremy G. Richman، نويسنده , , Daniel T. Connolly، نويسنده , , Graeme Semple، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
4
From page
5620
To page
5623
Abstract
A series of 5-alkyl pyrazole-3-carboxylic acids were prepared and found to act as potent and selective agonists of the human GPCR, GPR109a, the high affinity nicotinic acid receptor. No activity was observed at the highly homologous low affinity niacin receptor, GPR109b. A further series of 4-fluoro-5-alkyl pyrazole-3-carboxylic acids were shown to display similar potency. One example from the series was shown to have improved properties in vivo compared to niacin.
Keywords
PUMA-G , Niacin , GPR109A , lipolysis , Selectfluor , free fatty acids , GPCRs , Pyrazole carboxylic acids , Cutaneous flushing , HM74 , HM74a , GPR109b
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798666
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