PubMed · 2004 · 40 citations · 0 references
Life SciencesBiochemistryPharmacologyDrug DiscoveryLipid BiochemistryMolecular PharmacologyCardiovascular PharmacologyG Protein-coupled Receptor SignalingLipid MetabolismLipid-lowering TherapyLipoprotein MetabolismReceptor PharmacologyAdipocyte BiologyAdipocyte MetabolismG Protein-coupled Receptor ActivationG Protein-coupled Receptor BindingG Protein-coupled Receptor Control Of LipolysisMolecular Target SelectionNicotinic Receptor PharmacologyNormalization
Nicotinic acid has been used clinically for over 40 years in the treatment of dyslipidemia, producing a desirable normalization of a range of cardiovascular risk factors. The precise mechanism of action of nicotinic acid is unknown, although it is believed that activation of a Gi-type G protein-coupled receptor, resulting in the inhibition of adipocyte lipolysis, may contribute. This review describes the identification of this elusive receptor, and outlines the evidence suggesting that this may be the molecular target for the clinical effects of nicotinic acid.