Relatively high doses of nicotinic acid induce a profound change in the lipid and lipoprotein profile. In particular, the ability of nicotinic acid to decrease low-density lipoprotein cholesterol levels while increasing high-density lipoprotein cholesterol levels has led to its use as an antidyslipidemic drug. The mechanisms underlying the pharmacological effects of nicotinic acid have been unclear for decades. The recent discovery of a nicotinic acid receptor that is a G-protein-coupled receptor has led to a renewed interest in the pharmacological effects of nicotinic acid. This review summarizes recent progress in understanding the physiological and pharmacological role of the nicotinic acid receptor and discusses its potential use as a new target for the development of antidyslipidemic drugs to prevent and treat cardiovascular diseases.