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Nicotinic Acid Receptor
- Molecular classification
- G protein-coupled receptor
01
Overview
The nicotinic acid receptor family consists of three main subtypes: HCA1 (GPR81), HCA2 (GPR109A), and HCA3 (GPR109B). These are G protein-coupled receptors activated by nicotinic acid (niacin) and other hydroxycarboxylic acids. They play a key role in adipose tissue by modulating lipolysis, leading to antilipolytic effects and reducing the release of free fatty acids. They also have roles in anti-inflammatory processes and are therapeutic targets for metabolic and inflammatory diseases. Niacin's lipid-lowering effect is partly mediated through activation of these receptors, especially GPR109A/HCA2. HCA1 primarily responds to lactate.
- Other names
- Hydroxycarboxylic Acid ReceptorsHCARsHCA1GPR81HCA2GPR109AHCA3GPR109B
02
Mechanism of action
Activation inhibits adenylyl cyclase activity, leading to decreased cAMP levels within cells, resulting in reduced hormone-sensitive lipase activity and decreased fat breakdown.
03
Biological functions
Inhibition of adipocyte lipolysisModulation of inflammationLactate signaling
04
Disease associations
DyslipidemiaInflammationAtherosclerosisMetabolic disorders
05
Safety considerations
Niacin-induced flushingPotential for dysregulation of lipolysis
06
Interacting drugs
Niacin
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