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Discovery and development of TRPV1 antagonists
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Discovery and development of TRPV1 antagonists : ウィキペディア英語版
Discovery and development of TRPV1 antagonists
Relief from chronic pain remains a recognized unmet medical need. Consequently, the search for new analgesic agents is being intensively studied by the pharmaceutical industry. The TRPV1 receptor is an ion channel that has been implicated in mediation of many types of pain and therefore studied most extensively. The first competitive antagonist, capsazepine, was first described in 1990, since then development of novel TRPV1 antagonists has come a long way. This effort has led to the identification of several TRPV1 antagonists that have entered clinical trials as analgesic agents. Should these new chemical entities relieve symptoms of chronic pain then this class of compounds may offer one of the first novel mechanisms for the treatment of pain, in many years.〔〔
==History==

Capsaicin, the active ingredient in chilli pepper was first isolated over a century ago. In 1919 the exact chemical structure of capsaicin was determined and the complete synthesis of the compound was achieved a decade later. Capsaicin has been used as an analgesic for decades, but the therapeutic potential of capsaicin was first recognized as early as 1850. The effects of the pungent chemical, capsaicin, is mediated through the ligand gated ion channel TRPV1. This knowledge set the stage for further research of the function of the TRPV1 receptor and preclinical studies showed evidence of its importance in numerous human diseases.〔 These are the first agents acting by this mechanism that made their way into clinic for evaluation of their use as possible analgesics and therefore important targets for drug development. Many discoveries are yet to be made, both in terms of the range of potential therapeutic applications in addition to analgesia for TRPV1 antagonists and it was only in the last decade where there has been a full understanding of the molecular mechanism. In the years to come it will be clearer if TRPV1 antagonists can fulfill their potential.〔

抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
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