Turning up the Heat on Pain: TRPV1 Receptors in Pain and Inflammation

1. Front Matter

   Pages i-xii

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2. Historical perspective on capsaicin and its receptor

   1. Hot peppers, pain and analgesics

      • János Szolcsányi

      Pages 3-22

3. Molecular and cellular properties of vanilloid receptors

   1. Structural determinants of TRPV1 functionality

      • Makoto Tominaga

      Pages 25-37

   2. TRPV1 distribution and regulation

      • Janet Winter

      Pages 39-51

4. Pharmacology and physiology of vanilloid receptors

   1. Insights into TRPV1 pharmacology provided by non-capsaicin ligands

      • Peter M. Blumberg, Derek C. Braun, Noemi Kedei, Jozsef Lazar, Vladimir Pavlyukovets, Larry V. Pearce

      Pages 55-69

   2. Endocannabinoids and vanilloid TRPV1 receptors

      • Ruth A. Ross

      Pages 71-93

   3. Vanilloid receptor-mediated hyperalgesia and desensitization

      • Zoltán Sándor, Arpad Szallasi

      Pages 95-115

   4. Capsaicin in human experimental pain models of skin, muscle and visceral sensitization

      • Lars Arendt-Nielsen, Ole K. Andersen

      Pages 117-144

5. Vanilloid receptor involvement in disease states

   1. TRPV1 in gut function, abdominal pain and functional bowel disorders

      • Peter Holzer

      Pages 147-165

   2. TRPV1 in the airways

      • Maria G. Belvisi, Peter J. Barnes

      Pages 167-187

6. Therapeutic potential of vanilloid agonists and antagonists

   1. TRPV1 agonist-based therapies: mechanism of action and clinical prospects

      • Keith R. Bley, Annika B. Malmberg

      Pages 191-209

   2. TRPV1 agonist therapies in bladder diseases

      • Francisco Cruz, Carlos Silva, Paulo Dinis

      Pages 211-225

   3. TRPV1 antagonists and chronic pain

      • Kenneth J. Valenzano, James D. Pomonis, Katharine Walker

      Pages 227-243

7. Back Matter

   Pages 245-252

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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.

• Activation
• analgesics
• cannabinoid
• diseases
• drug
• drug development
• inflammation
• lead
• muscle
• neurons
• pain
• pharmacology
• physiology
• regulation
• treatment

• Elan Pharmaceuticals, South San Francisco, USA

  Annika B. Malmberg

• NeurogesX, Inc., San Carlos, USA

  Keith R. Bley

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