Vanilloid Receptor TRPV1 in Drug Discovery: Targeting Pain and Other Pathological Disorders / Edition 1

by Arthur Gomtsyan, Connie R. Faltynek

Overview

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.

Product Details

ISBN-13:	9780470175576
Publisher:	Wiley
Publication date:	03/01/2010
Pages:	480
Product dimensions:	6.20(w) x 9.30(h) x 1.10(d)

About the Author

ARTHUR GOMTSYAN is an Associate Research Fellow at Abbott Laboratories where he focuses on neuroscience research and pain drug targets. He is on the editorial board of two peer-reviewed journals and has over forty scientific articles to his credit.

CONNIE R. FALTYNEK is a Director for Neuroscience and Pain Discovery at Abbott Laboratories. She has twenty years' experience in drug discovery research in the pharmaceutical industry and has published nearly 100 scientific papers.

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Table of Contents

Preface And Acknowledgments ix

Foreword xiii

Contributors xv

Part I Introduction to the TRP Channels 1

1 TRP Channels and Human Diseases Bernd Nilius Rudi Vennekens 3

2 Role of TRP Channels in Pain: An Overview Arpad Szallasi 68

3 Biochemical Pharmacology of TRPV1: Molecular Integrator of Pain Signals Carol S. Surowy Philip R. Kym Regina M. Reilly 101

4 TRPV1 Genetics Ruslan Dorfman Hubert Tsui Michael W. Salter H.-Michael Dosch 134

Part II Role For TRPV1 in Pain States 151

5 TRPV1 and Inflammatory Pain Anindya Bhattacharya Sonya G. Lehto Narender R. Gavva 153

6 Role of TRPV1 Receptors in Osteoarthritic Pain Shailen K. Joshi Prisca Honore 175

7 TRPV1 and Bone Cancer Pain Juan Miguel Jimenez-Andrade Patrick Mantyh 191

8 TRPV1 in Visceral Pain and Other Visceral Disorders António Avelino Francisco Cruz 206

9 TRPV1 Receptors and Migraine Philip R. Holland Peter J. Goadsby 239

10 TRPV1 in Neuropathic Pain and Neurological and Neuropsychiatric Disorders Enza Palazzo Katarzyna Starowicz Sabatino Maione Vincenzo Di Marzo 260

Part III TRPV1 Antagonists and Agonists as Novel Analgesic Drugs 293

11 Aryl-Urea Class and Related TRPV1 Antagonists Arthur Gomtsyan 295

12 2-Pyridinylpiperazine Carboxamide Class and Related TRPV1 Antagonists Natalie A. Hawryluk Nicholas I. Carruthers 311

13 TRPV1 Agonist Approaches for Pain Management Keith R. Bley 325

Part IV Role For TRPV1 in Other Physiological Processes Besides Pain Transmission 349

14 The TRPV1 Channel in Normal Thermoregulation: What Have We Learned from Experiments Using Different Tools? Andras Garami Maria C. Almeida Tatiane B. Nucci Tamara Hew-Butler Renato N. Soriano Eszter Pakai Kazuhiro Nakamura Shaun F. Morrison Andrej A. Romanovsky 351

15 The Role of TRPV1 in Respiratory Diseases Serena Materazzi Alain Tchoimou Romina Nassini Marcello Trevisani Pierangelo Geppetti 403

16 The Role of TRPV1 in Diabetes Hubert Tsui Ruslan Dorfman Michael W. Salter H.-Michael Dosch 423

Afterword 449

Index 451