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Role of Transient Receptor Potential Vanilloid 1 in Inflammation and Autoimmune Diseases
Research and Development Center, Santen Pharmaceutical Co., Ltd., 8916-16 Takayama-cho, Ikoma, Nara 630-0101, Japan
* Author to whom correspondence should be addressed.
Received: 29 June 2012; in revised form: 2 August 2012 / Accepted: 15 August 2012 / Published: 17 August 2012
Abstract: Transient receptor potential vanilloid 1 (TRPV1), a non-selective cation channel, is a receptor activated by high temperatures and chemical agonists such as the vanilloids and protons. Because of these properties, TRPV1 has emerged as a polymodal nocisensor of nociceptive afferent neurons. TRPV1 is thought to be a central transducer of hyperalgesia and a prime target for controlling pain pharmacologically because it is a point where many proalgesic pathways converge and it is upregulated and sensitized by inflammation and injury. However, whether TRPV1 agonists promote or inhibit inflammation remains unclear. We recently demonstrated that SA13353 (1-[2-(1-adamantyl)ethyl]-1-pentyl-3-[3-(4-pyridyl)propyl]urea), a novel TRPV1 agonist, inhibits tumor necrosis factor-a production by the activation of capsaicin-sensitive afferent neurons and reduces the severity of symptoms in kidney injury, lung inflammation, arthritis, and encephalomyelitis. These results suggest that TRPV1 agonists may act as anti-inflammatories in certain inflammatory and autoimmune conditions in vivo. Given the potential deleterious effects of inhibiting the population of channels with a protective function, caution should be taken in the use of potent TRPV1 antagonists as a general strategy to treat inflammation. Further studies are required to clarify the role of TRPV1 and neuropeptides, which are released because of TRPV1 activation in inflammation and autoimmune diseases.
Keywords: SA13353; transient receptor potential vanilloid 1; kidney injury; lung inflammation; autoimmune diseases; pain
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MDPI and ACS Style
Tsuji, F.; Aono, H. Role of Transient Receptor Potential Vanilloid 1 in Inflammation and Autoimmune Diseases. Pharmaceuticals 2012, 5, 837-852.
Tsuji F, Aono H. Role of Transient Receptor Potential Vanilloid 1 in Inflammation and Autoimmune Diseases. Pharmaceuticals. 2012; 5(8):837-852.
Tsuji, Fumio; Aono, Hiroyuki. 2012. "Role of Transient Receptor Potential Vanilloid 1 in Inflammation and Autoimmune Diseases." Pharmaceuticals 5, no. 8: 837-852.