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Vanilloid Receptor TRPV1 in Drug Discovery (eBook)

Targeting Pain and Other Pathological Disorders
eBook Download: PDF
2010
John Wiley & Sons (Verlag)
978-0-470-58827-7 (ISBN)

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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.

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.


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 "e;the holy grail"e; 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.

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.

VANILLOID RECEPTOR TRPV1 IN DRUG DISCOVERY 3
CONTENTS 9
PREFACE AND ACKNOWLEDGMENTS 11
FOREWORD 15
CONTRIBUTORS 17
PART I INTRODUCTION TO THE TRP CHANNELS 21
1 TRP Channels and Human Diseases 23
2 Role of TRP Channels in Pain: An Overview 88
3 Biochemical Pharmacology of TRPV1: Molecular Integrator of Pain Signals 121
4 TRPV1 Genetics 154
PART II ROLE FOR TRPV1 IN PAIN STATES 171
5 TRPV1 and Inflammatory Pain 173
6 Role of TRPV1 Receptors in Osteoarthritic Pain 195
7 TRPV1 and Bone Cancer Pain 211
8 TRPV1 in Visceral Pain and Other Visceral Disorders 226
9 TRPV1 Receptors and Migraine 259
10 TRPV1 in Neuropathic Pain and Neurological and Neuropsychiatric Disorders 280
PART III TRPV1 ANTAGONISTS AND AGONISTS AS NOVEL ANALGESIC DRUGS 313
11 Aryl-Urea Class and Related TRPV1 Antagonists 315
12 2-Pyridinylpiperazine Carboxamide Class and Related TRPV1 Antagonists 331
13 TRPV1 Agonist Approaches for Pain Management 345
PART IV ROLE FOR TRPV1 IN OTHER PHYSIOLOGICAL PROCESSES BESIDES PAIN TRANSMISSION 369
14 The TRPV1 Channel in Normal Thermoregulation: What Have We Learned from Experiments Using Different Tools? 371
15 The Role of TRPV1 in Respiratory Diseases 423
16 The Role of TRPV1 in Diabetes 443
AFTERWORD 469
INDEX 471

Erscheint lt. Verlag 12.2.2010
Sprache englisch
Themenwelt Medizin / Pharmazie Gesundheitsfachberufe
Medizin / Pharmazie Medizinische Fachgebiete Pharmakologie / Pharmakotherapie
Naturwissenschaften Chemie
Schlagworte available • Biowissenschaften • Chemie • Chemistry • chronic low • Contributions • Data • dedicated • Drug Discovery & Development • Experts • Integrator • Life Sciences • Ligands • Managing • many • Medical Science • Medizin • Multiple • Neuroscience • Neurowissenschaften • noxious • Pharmacology & Pharmaceutical Medicine • Pharmakologie u. Pharmazeutische Medizin • Pharmazeutische Chemie • Potential • reference summarizes • Role • Stimuli • Therapeutic • TRP Channels • trpv • Types • Utility • Wirkstoffforschung • Wirkstoffforschung u. -entwicklung • Worlds
ISBN-10 0-470-58827-6 / 0470588276
ISBN-13 978-0-470-58827-7 / 9780470588277
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