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Publication : Molecular identification of nicotinic acid receptor.

First Author  Soga T Year  2003
Journal  Biochem Biophys Res Commun Volume  303
Issue  1 Pages  364-9
PubMed ID  12646212 Mgi Jnum  J:82939
Mgi Id  MGI:2656085 Doi  10.1016/s0006-291x(03)00342-5
Citation  Soga T, et al. (2003) Molecular identification of nicotinic acid receptor. Biochem Biophys Res Commun 303(1):364-9
abstractText  Nicotinic acid and its derivative, Acipimox, have been widely used in the treatment of hyperlipidemia. Pharmacological studies have demonstrated that they exert the beneficial effect through the activation of a Gi-protein-coupled receptor on adipocyte, which has remained elusive to date. Here we show that a novel GPCR, designated HM74b because of its high similarity to HM74, is a receptor for nicotinic acid. HM74b mRNA is found in human, murine, and rat adipose tissues. Nicotinic acid and Acipimox inhibit forskolin-stimulated intracellular cAMP accumulation in human HM74b-expressing cells and activate GTP gamma S binding in a dose-dependent manner. [3H]Nicotinic acid specifically binds to HM74b-expressing membrane and its binding is replaced by Acipimox. This finding will open a new phase of research on the physiological role of nicotinic acid and will be a clue to develop novel antihyperlipidemic drugs.
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