Offermanns Stefan
Institute of Pharmacology, University of Heidelberg, Im Neuenheimer Feld 366, 69120 Heidelberg, Germany.
Trends Pharmacol Sci. 2006 Jul;27(7):384-90. doi: 10.1016/j.tips.2006.05.008.
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.
相对高剂量的烟酸会引起脂质和脂蛋白谱的深刻变化。特别是，烟酸降低低密度脂蛋白胆固醇水平同时升高高密度脂蛋白胆固醇水平的能力，使其被用作抗血脂异常药物。几十年来，烟酸药理作用的潜在机制一直不清楚。最近发现烟酸受体是一种G蛋白偶联受体，这引发了人们对烟酸药理作用的新兴趣。这篇综述总结了在理解烟酸受体的生理和药理作用方面的最新进展，并讨论了其作为开发预防和治疗心血管疾病的抗血脂异常药物新靶点的潜在用途。
