jksh Journal of the Korean Society of Hypertension J Korean Soc Hypertens 2233-8136 2233-8454 The Korean Society of Hypertension 10.5646/jksh.2011.17.2.37 jksh-17-37 Review Transient Receptor Potential Vanilloid Type-1 Channel in Cardiometabolic Protection WangPeijian LiuDaoyanPhD ZhuZhimingMD Department of Hypertension and Endocrinology, Centre for Hypertension and Metabolic Diseases, Daping Hospital, Third Military Medical University, Chongqing Institute of Hypertension, Chongqing, China Department of Hypertension and Endocrinology, Centre for Hypertension and Metabolic Diseases, Daping Hospital, Third Military Medical University, Chongqing Institute of Hypertension, Chongqing 400042, China Tel: +86-23-6875 7889, Fax: +86-23-69705094 E-mail: zhuzm@yahoo.com 06 2011 10 06 2011 17 2 37 47 16122010 13062011 14062011 Copyright © 2011 The Korean Society of Hypertension 2011 This is an Open Access article distributed under the terms of the Creative Commons Attribution Non-Commercial License (http://creativecommons.org/licenses/by-nc/3.0/) which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited. ABSTRACT

Transient receptor potential vanilloid type-1 channel (TRPV1) is a non-selective cation channel with a preference for calcium ions that is able to sense a vast range of endogenous physical and chemical stimuli and plays an important role in transducing the sensations of noxious heat and pain signaling. Recent studies showed that TRPV1 is widely expressed in different tissues and organs beyond the sensory nerves and has multiple biological effects that are involved in functional regulation in the pancreas, blood vessel, adipose tissue and liver. To further understand the link between TRPV1 and cardiometabolic diseases, we reviewed the role of TRPV1 in hypertension, diabetes, obesity, and dyslipidemia. This review provides new insights into the involvement of TRPV1 channels in the pathogenesis of cardiometabolic disorders and implicates this channel as a potential therapeutic target for the management of cardiometabolic diseases.

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Transient receptor potential vanilloid type-1 channel (TRPV1) has six transmembrane domains and a short, pore-forming hydrophobic stretch between the fifth and sixth transmembrane domains. Capsaicin binding to TRPV1 triggers an increase in intracellular calcium. When this occurs in sensory nerves, it promotes the sensation of pain, inflammation, and local heat. TRPV1 is also activated by noxious heat (>43°C) and acid (pH<5.9), voltage, and various lipids.

Transient receptor potential vanilloid type-1 channel (TRPV1) is widely expressed in the car-diometabolic system such as in pancreas, blood vessels, adipose tissue and liver. Activation of TRPV1 causes the relaxation of arteries leading to a decrease in blood pressure; increases the secretion of insulin from islet β cells and lowers blood glucose; improves insulin resistance; reduces inflammation, triglycerides, cholesterol, and adipogenesis; increases thermogenesis; and prevents obesity, implying that activation of TRPV1 will decrease cardiometabolic risk.