Identification of a nicotinic acid receptor: is this the molecular target for the oldest lipid-lowering drug?

Curr Opin Investig Drugs. 2004 Mar;5(3):271-5.


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.

Publication types

  • Review

MeSH terms

  • Animals
  • Drug Delivery Systems
  • Furans / chemistry
  • Furans / pharmacology
  • Humans
  • Hypolipidemic Agents / chemistry
  • Hypolipidemic Agents / pharmacology*
  • Ligands
  • Niacin / chemistry
  • Niacin / pharmacology*
  • Receptors, G-Protein-Coupled
  • Receptors, Nicotinic / drug effects*
  • Receptors, Nicotinic / metabolism


  • Furans
  • HCAR3 protein, human
  • Hypolipidemic Agents
  • Ligands
  • Receptors, G-Protein-Coupled
  • Receptors, Nicotinic
  • Niacin
  • acifran