Pike Nicholas B, Wise Alan
Cardiovascular and Urogenital Centre of Excellence for Drug Discovery, GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, SG1 2NY, UK.
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.
烟酸已在临床上用于治疗血脂异常40多年,可使一系列心血管危险因素实现理想的正常化。尽管人们认为激活一种Gi型G蛋白偶联受体,从而抑制脂肪细胞脂解可能起了作用,但烟酸的确切作用机制尚不清楚。这篇综述描述了这种难以捉摸的受体的鉴定过程,并概述了表明其可能是烟酸临床效应分子靶点的证据。