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Niacin receptor 1

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Title: Niacin receptor 1  
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Subject: High-density lipoprotein
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Niacin receptor 1

Hydroxycarboxylic acid receptor 2
HCAR2 Gene

Niacin receptor 1, also known as NIACR1 or GPR109A, is a protein which in humans is encoded by the NIACR1 gene.[1][2][3][4]


GPR109A is a high affinity receptor for nicotinic acid (niacin)[3][4] and is a member of the nicotinic acid receptor family of G protein-coupled receptors (the other identified member being GPR109B).

GPR109A is a Gi / Go protein-coupled receptor with high affinity for nicotinic acid.[3]

Clinical significance

GPR109A is believed to be an important biomolecular target of niacin which is a widely prescribed drug for the treatment of dyslipidemia and to increase HDL cholesterol but whose therapeutic use is limited by flushing.[5] In GPR109A knockout mice, the effects of niacin on both lipids[6] and flushing[7] is eliminated. Furthermore in arrestin beta 1 knockout mice, niacin's effect on flushing is greatly reduced while the lipid modifying effects are maintained.[8]

The precise mechanism of action of niacin therapeutic effects has not been fully elucidated but appears to work in part through activation of GPR109A which reduces the levels of intracellular cAMP thereby inhibiting lipolysis in adipocytes.[9] In contrast, the flushing effect is due to GPR109A activation of ERK 1/2 MAP kinase[10] mediated by arrestin beta 1.[8] Activation of MAP kinase in turn causes release of prostaglandin D2 from Langerhans cells in the skin.[11]


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