Molecular identification of nicotinic acid receptor
T Soga, M Kamohara, J Takasaki, S Matsumoto… - Biochemical and …, 2003 - Elsevier
T Soga, M Kamohara, J Takasaki, S Matsumoto, T Saito, T Ohishi, H Hiyama, A Matsuo…
Biochemical and biophysical research communications, 2003•ElsevierNicotinic 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 …
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 …
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 GTPγS 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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