Structure, function, and mechanism of action of the vanilloid TRPV1 receptor

Abstract

The TRPV1 receptor (transient receptor potential cation channel subfamily V member 1) is a non-selective cationic channel activated by vanilloids like capsaicin. Therefore, TRPV1 is also called a capsaicin’s receptor, which is a spicy substance found in chili peppers. The receptor is located in sensory nerve fibers and non-neuronal cells, for example in vascular endothelial and smooth muscle cells. It is thought to act as an integrator of various physical and chemical stimuli that provide heat and pain. The activation of the TRPV1 may affect at various physiological functions like release inflammatory mediators, gastrointestinal motility and temperature regulation. Numerous studies in recent years show TRPV1 plays an important role in physiology and development of pathological conditions of gastrointestinal, cardiovascular and respiratory system. These receptors are widely studied as a gripping point for new painkillers, but there are also data indicating their potential involvement in the pathomechanism of various diseases, e.g. epilepsy. TRPV1 targeting may be useful not only in paintreatment but also urinary incontinence, chronic cough or irritable bowel syndrome. The need for further investigation of the therapeutic potential of TRPV1 antagonists indicates the lack of effective drugs to treat many of these conditions. The purpose of this article is to collect and summarize knowledge about the TRPV1 receptor, its structure and mechanism of action.