Bibliothèque de L'IMIST/CNRST

Vanilloids mediate their effects by selective agonism of an ion channel, the vanilloid receptor 1 (TRPV1). TRPV1 is a ligand-gated, non-selective, cation channel preferentially expressed in small-diameter, primary afferent neurons, including nociceptive sensory nerves. In addition to be activated by capsaicin and related vanilloids, TRPV1 responds to heat and extracellular acidification, and will integrate simultaneous exposures to these stimuli. The aim of this book is to summarize recent insights in the role of TRPV1 in pain and inflammation, and to discuss how modulation of this receptor may lead to important advances in analgesic drug development. Insights into the prospects for the therapeutic potential of TRPV1 activation or inhibition, particularly in various painful or inflammatory conditions, are provided. The volume is written for basic scientists and clinicians interested in the mechanisms of pain, inflammation and the treatment of these conditions.

Includes bibliographical references and index.

Part I: Historical perspective on capsaicin and its receptor -- Hot peppers, pain and analgesics -- Part II: Molecular and cellular properties of vanilloid receptors -- Structural determinants of TRPV1 functionality -- TRPV1 distribution and regulation -- Part III: Pharmacology and physiology of vanilloid receptors -- Insights into TRPV1 pharmacology provided by non-capsaicin ligands -- Endocannabinoids and vanilloid TRPV1 receptors -- Vanilloid receptor-mediated hyperalgesia and desensitization -- Capsaicin in human experimental pain models of skin, muscle and visceral sensitization -- Part IV: Vanilloid receptor involvement in disease states -- TRPV1 in gut function, abdominal pain and functional bowel disorders -- TRPV1 in the airways --- Part V: Therapeutic potential of vanilloid agonists and antagonists -- TRPV1 agonist-based therapies: mechanism of action and clinical prospects -- TRPV1 agonist therapies in bladder diseases -- TRPV1 antagonists and chronic pain.