Examines the emerging therapeutic role of TRPV1 TRPV1 is considered an integrator of noxious stimuli and therefore may be at a crossroads for pain transmission pathways. Because of its potential for managing multiple pain types, including osteoarthritis, chronic low back pain, neuropathic pain, and cancer pain, some consider it "the holy grail" of pain management. This dedicated reference summarizes available data related to the potential therapeutic utility for TRPV1 ligands. With contributions from many of the world's leading experts on TRP channels, Vanilloid Receptor TRPV1 in Drug Discovery covers the important TRPV1 target for drugs to treat painful conditions such as inflammation, arthritis, and cancer pain. The book discusses: Recent advances in biology, chemistry, and pharmacology at both the preclinical and clinical stage of the dynamic area of TRPV1 drug discovery research The potential for drugs targeting TRPV1 in painful conditions such as inflammation, arthritis, and cancer The development of analgesic drugs Other applications for TRPV1, including the treatment of respiratory disease and diabetes Featuring data relevant to the therapeutic potential of TRPV1 and the medicinal chemistry involved in designing TRPV1 antagonists, Vanilloid Receptor TRPV1 in Drug Discovery is a key tool for researchers in the pharmaceutical industry and academia involved in pain, ion channels, and analgesic drug development.

This book is a printed edition of the Special Issue "Transient Receptor Potential (TRP) Channels in Drug Discovery: Old Concepts & New Thoughts" that was published in Pharmaceuticals

Since the first TRP ion channel was discovered in Drosophila melanogaster in 1989, the progress made in this area of signaling research has yielded findings that offer the potential to dramatically impact human health and wellness. Involved in gateway activity for all five of our senses, TRP channels have been shown to respond to a wide range of st

TRP Channels as Therapeutic Targets: From Basic Science to Clinical Use is authored by experts across academia and industry, providing readers with a complete picture of the therapeutic potential and challenges associated with using TRP channels as drug targets. This book offers a unique clinical approach by covering compounds that target TRP channels in pre-clinical and clinical phases, also offering a discussion of TRP channels as biomarkers. An entire section is devoted to the novel and innovative uses of these channels across a variety of diseases, offering strategies that can be used to overcome the adverse effects of first generation TRPV1 antagonists. Intended for all researchers and clinicians working toward the development of successful drugs targeting TRP channels, this book is an essential resource chocked full of the latest clinical data and findings. Contains comprehensive coverage of TRP channels as therapeutic targets, from emerging clinical indications to completed clinical trials Discusses TRP channels as validated targets, ranging from obesity and diabetes through cancer and respiratory disorders, kidney diseases, hypertension, neurodegenerative disorders, and more Provides critical analysis of the complications and side effects that have surfaced during clinical trials, offering evidence-based suggestions for overcoming them

Despite tremendous advances in the understanding of the sensory nervous system which have accompanied the recent explosive growth of the neurosciences, rema- ably few innovative medicines directed towards pain and inflammation are ava- able. Indeed, many patients are still prescribed analgesic and anti-inflammatory medications that were identified long ago as components of herbal remedies. Si- larly, potential new medicines in clinical evaluation based on capsaicin and the c- saicin receptor are both grounded firmly on folk traditions and yet rely upon the most contemporary techniques of drug discovery and delivery. The first formal report of the pain-relieving properties of capsaicin appeared in 1850 [1]. However, for centuries before this, capsaicin-containing extracts had been used as folk medicines in cultures with access to pepper plants, much in the same way as poppy or willow-bark extracts were. Despite widespread use, it was not until 1878 that the selective action of capsaicin on the sensory nervous system was r- ognized [2]. In Chapter 1 of this volume, Janos Szolcsányi reviews this early research, which culminated with the seminal studies of Nicholas Jansco and his c- leagues in Hungary in the 1940s. Since then, capsaicin and related vanilloid c- pounds have played a prominent role in analgesia and inflammation investigations because of their ability to selectively activate a subpopulation of sensory neurons and produce sensations of pain and localized erythema.

This volume provides up-to-date information on the molecular and functional properties and pharmacology of mammalian TRP channels. Leading experts in the field have written 35 essays which describe properties of a single TRP protein/channel or portray more general principles of TRP function and important pathological situations linked to mutations of TRP genes or their altered expression.