TRP Channels as Therapeutic Targets

TRP Channels as Therapeutic Targets

From Basic Science to Clinical Use

1st Edition - March 14, 2015

Write a review

  • Editor: Arpad Szallasi
  • eBook ISBN: 9780124200791
  • Hardcover ISBN: 9780124200241

Purchase options

Purchase options
DRM-free (Mobi, EPub, PDF)
Sales tax will be calculated at check-out

Institutional Subscription

Free Global Shipping
No minimum order


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.

Key Features

  • 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


New and established researchers from academia and industry involved in target validation, compound discovery and drug development programs aimed at TRP channels; clinical investigators/clinicians who need to become familiar with the latest clinical trials with drugs targeting TRP channels

Table of Contents

    • Preface
    • Chapter 1: An Introduction to Transient Receptor Potential Ion Channels and Their Roles in Disease
      • Abstract
      • Discovery and General Properties of TRP Channels
      • TRP Channels in Normal Physiology
      • TRP Channels and Disease
      • Therapeutic Strategies Based on TRP Channel Modulation
      • Acknowledgment
    • Chapter 2: Transient Receptor Potential Dysfunctions in Hereditary Diseases: TRP Channelopathies and Beyond
      • Abstract
      • Acknowledgments
      • Introduction
      • TRPC Channelopathies
      • TRPV Channelopathies
      • TRPM Channelopathies
      • TRPA Channelopathies
      • TRPML Channelopathies
      • TRPP Channelopathies
      • Conclusions
    • Chapter 3: The Role of TRPV1 in Acquired Diseases: Therapeutic Potential of TRPV1 Modulators
      • Abstract
      • Acknowledgment
      • Introduction
      • TRPV1 and Pain
      • TRPV1 and Gastrointestinal System-Related Disease
      • TRPV1 and Urinary System-Related Diseases
      • TRPV1 and Central Nervous System-Related Diseases
      • TRPV1 and Respiratory System-Related Diseases
      • TRPV1 and Cancer
      • TRPV1 and Cardiovascular System-Related Diseases
      • TRPV1 and Metabolic Diseases
      • TRPV1 and Other Disease Conditions
      • Conclusions
    • Chapter 4: TRP Gene Polymorphism and Disease Risk
      • Abstract
      • TRP Gene Polymorphism
      • TRPA1
      • The TRPC Subfamily
      • The TRPM Subfamily
      • The TRPML Subfamily
      • The TRPV Subfamily
      • Disease Risk, Clinical Diagnosis, and Personalized Medicine
    • Chapter 5: Use of Topical Capsaicin for Pain Relief
      • Abstract
      • Introduction
      • Pharmacodynamics
      • Pharmacokinetics
      • Efficacy and Therapeutic Uses
      • Safety and Tolerability
      • Delivery of Treatment with Capsaicin 8% Patch—Practical Aspects
      • Application Procedure for the Capsaicin 8% Patch
      • Postprocedural Instructions for Patients
    • Chapter 6: TRPV1 Agonist Cytotoxicity for Chronic Pain Relief: From Mechanistic Understanding to Clinical Application
      • Abstract
      • Introduction
      • Mechanisms of TRPV1 Agonist Therapeutic Action
      • Four Main Determinants of TRPV1 Agonist Actions
      • Selectivity of RTX at the Cellular Level
      • RTX Produces a Prolonged Channel Open Time
      • TRPV1 Is Selectively Expressed in Subpopulations of DRG Neurons
      • RTX Is Administered Locally
      • Companion Dog and Human Studies
      • Companion (Pet) Dog Models of Chronic Pain
      • TRPV1 Agonists in the Companion Dog Model of Bone Cancer
      • TRPV1 Agonists in the Companion Dog Model of Osteoarthritis
      • Human Studies
    • Chapter 7: Intravesical Capsaicin and Resiniferatoxin for Bladder Disorders
      • Abstract
      • Capsaicin and Resiniferatoxin Targets and Effects in the Urinary Bladder
      • The Rationale for Using Vanilloids to Overcome Lower Urinary Tract Symptoms
      • Intravesical Application of Vanilloids
      • Is There a Future for Intravesical Instillation of Vanilloids in the Urinary Bladder?
    • Chapter 8: Clinical and Preclinical Experience with TRPV1 Antagonists as Potential Analgesic Agents
      • Abstract
      • Introduction
      • Preclinical Overview of TRPV1 Antagonists
      • Clinical Overview of TRPV1 Antagonists
      • Perspective
    • Chapter 9: Transient Receptor Potential Ankyrin 1 Channel Antagonists for Pain Relief
      • Abstract
      • Acknowledgments
      • Introduction
      • General Properties of the TRPA1 Channel in Pain Transduction and Amplification
      • TRPA1 in Pathophysiological Pain Models
      • Biomarkers
      • Conclusions
    • Chapter 10: TRPA1 Antagonists as Potential Therapeutics for Respiratory Diseases
      • Abstract
      • TRPA1 as a Reactive, Noxious Irritant Sensor
      • Presence and Function of TRPA1 in the Mammalian Respiratory Tract
      • Exogenous Agonists that Cause TRPA1 Activation in the Airways
      • Non-Aldehyde TRPA1 Agonists Found in Cigarette Smoke
      • Other Hazardous Air Pollutants that Activate TRPA1
      • Endogenous Molecules that Signal Through TRPA1 in Mammals
      • Nonneuronal TRPA1 Expression and Function
      • In Vivo Preclinical Pharmacology of TRPA1 Blockers
      • TRPA1 Antagonists Claimed in the Patent Literature
      • Conclusions
    • Chapter 11: Is TRPV3 a Drug Target?—A Decade of Learning
      • Abstract
      • Introduction
      • TRPV3 Tissue Expression
      • TRPV3 Activation
      • Functional Role of TRPV3 Channel: Evidence from Genetic Studies
      • TRPV3 and Human Diseases
      • Safety of TRPV3 Antagonists
      • Pharma Efforts in Discovering TRPV3 Antagonists in Treatment of Human Diseases
    • Chapter 12: Small Molecule Agonists and Antagonists of TRPV4
      • Abstract
      • Introduction
      • TRPV4 Agonists
      • TRPV4 Antagonists
      • Conclusions
    • Chapter 13: Potential Therapeutic Applications for TRPV4 Antagonists in Lung Disease
      • Abstract
      • Introduction
      • TRPV4 Localization in Lungs
      • Acute Lung Injury via Direct Channel Activation
      • Ventilator-Induced Lung Injury (VILI)
      • High Vascular Pressure-Induced Lung Injury
      • Heart Failure and Pulmonary Edema
      • Pulmonary Arterial Hypertension
      • Airway Disease and Cough
    • Chapter 14: TRPM8 as a Target for Analgesia
      • Abstract
      • TRPM8 Structure
      • Localization of TRPM8 in the Nervous System
      • In Vitro Studies on the Physiological Role of TRPM8 in Sensing Cool/Cold Temperatures
      • In Vivo Studies on the Physiological Role of TRPM8 in Sensing Cool/Cold Temperatures
      • Setting of Thermal Sensitivity in TRPM8-Expressing Sensory Neurons
      • The Impact of Pain States on TRPM8 Function
      • TRPM8-Mediated Analgesia
      • TRPM8 in Thermoregulation
      • Pharmacology of TRPM8 Antagonists and Agonists
      • Modulation of TRPM8 Function by Cellular Signaling
      • CNS Processes Activated by TRPM8-Positive Afferents
      • Conclusions
    • Chapter 15: Connecting TRP Channels and Cerebrovascular Diseases
      • Abstract
      • Overview: TRP Channels: Types, Distribution, and Function
      • TRP Channels in Diseases
      • TRP Channels in Smooth Muscle Cells
      • TRP Channels and Endothelial Function
      • TRP Channels and Hypertension
      • TRP Channels and Stroke
      • Future Directions
    • Chapter 16: Activating, Inhibiting, and Highjacking TRP Channels for Relief from Itch
      • Abstract
      • Introduction
      • Which Sensory Neurons Signal Itch?
      • Activating TRP Channels to Block Itch
      • Inhibiting TRP Channels to Block Itch
      • Highjacking TRP Channels to Deliver Relief from Itch
      • An Unexpected Role for TprV3: Mutations in TRPV3 Result in Itchy Lesions Found in Olmsted Syndrome
      • Conclusions
    • Chapter 17: Role of TRP Channels in Skin Diseases
      • Abstract
      • Introduction
      • TRPV Subfamily
      • TRPA1
      • The TRPC (Canonical) Family
      • TRPMs
      • TRPML3
      • Summary
    • Chapter 18: Transient Receptor Potential Channels in Hypertension and Metabolic Syndrome
      • Abstract
      • TRP Channels in Hypertension
      • TRP Channels in Metabolic Syndrome
      • Perspective
    • Chapter 19: Transient Receptor Potential (TRP) Cation Channels in Diabetes
      • Abstract
      • Acknowledgments
      • TRP’s in Pancreatic ß Cells
      • TRPV1-Expressing Sensory Neurons in β Cell Function and Diabetes Mellitus
      • TRP Channels in Diabetes-Associated Complications
      • TRP Channels as Drug Target in T1DM and T2DM
      • Conclusions
    • Chapter 20: TRP Channels in Cardiovascular Disease
      • Abstract
      • Acknowledgment
      • Calcium Signaling in the Cardiovascular System
      • TRP Channels and Cardiovascular Disease
      • TRP Channels in Cardiac Hypertrophy
      • Role of TRP Channels in Cardiac Hypertrophy Signaling Pathways
      • Pharmacological Developments Targeting TRP Channels in Cardiac Hypertrophy
      • TRP Channels and Cardiac Arrhythmias
      • TRPM4 and Cardiac Conduction Disease
      • TRPM7 Channels and Atrial Fibrillation
      • TRPC Channels in Pulmonary Hypertension
    • Chapter 21: Targeting of Transient Receptor Potential Channels in Digestive Disease
      • Abstract
      • Acknowledgments
      • Overview
      • Expression of TRP Channels in the Gut and Their Role in GI Motility and Secretion
      • TRP Channels as Targets for Prokinetic Drugs
      • Roles of TRP Channels in the Development of IBD
      • TRP Channel Sensitization in IBS- and IBD-Related Pain
      • Summary
    • Chapter 22: TRP Channels in Cancer
      • Abstract
      • Introduction
      • The Role of TRP Channels in Cancer
      • Clinical Implications and Concluding Remarks
    • Chapter 23: Are Brain TRPs Viable Targets for Curing Neurodegenerative Disorders and Improving Mental Health?
      • Abstract
      • The Role of TRP Channels in Building the Brain and Regulating its Functions: Introducing the Players
      • TRP Channel Dysfunction in Epilepsy
      • Cerebellar Ataxia as a “TRP Channelopathy”
      • TRP Channels in Neuroprotection and Their Dysfunction in Neurodegenerative Disorders
      • TRP Channels in Psychiatric Disorders and Mental Retardation
      • The “Addictive” TRP Channels
      • TRP Channels in Stroke and Traumatic Brain Injury
      • Conclusions
    • Chapter 24: Mucolipidosis Type IV: Part I
      • Abstract
      • Introduction
      • Clinical Presentation
      • Cellular Abnormalities in MLIV Patients
      • MCOLN1 and Mucolipin-1
      • Mutations in the MCOLN1 gene
      • The Mucolipin Channel and its Interacting Partners
      • Animal Models for MLIV
      • Summary and Future Goals
    • Chapter 25: TRPML1-Dependent Processes as Therapeutic Targets
      • Abstract
      • Acknowledgments
      • Introduction
      • TRPML1 Features and Properties
      • TRPML1-Dependent Processes, Shown and Discussed
      • TRPML1-Dependent Processes Inferred from its Functional Context
      • Conclusions
    • Chapter 26: TRPs in Respiratory Disorders: Opportunities Beyond TRPA1
      • Abstract
      • Introduction
      • Overview of TRP Channels and Their Expression and Function in the Respiratory System
      • Summary and Perspectives
    • Chapter 27: Conclusions
    • Index

Product details

  • No. of pages: 536
  • Language: English
  • Copyright: © Academic Press 2015
  • Published: March 14, 2015
  • Imprint: Academic Press
  • eBook ISBN: 9780124200791
  • Hardcover ISBN: 9780124200241

About the Editor

Arpad Szallasi

Arpad Szallasi is a leading expert on the roles of TRP channels in health and disease. He was the first to provide a biochemical proof for the existence of the vanilloid (capsaicin) receptor, now known as TRPV1. Currently, he holds an Associate Professor position at the 1st Department of Pathology and Experimental Cancer Research, Semmelweis University, Budapest, Hungary. His research focuses on targeting of TRP channels for therapeutic purposes, with special emphasis on pain and inflammation. Arpad Szallasi obtained his MD degree Summa cum Laude from the Medical University School of Debrecen, Hungary (1984). He received his PhD degree in Pharmacology from the Karolinska Institute, Stockholm, Sweden (1995). Arpad Szallasi held several research positions both in academia (Karolinska Institute, Washington University, St. Louis, MO) and industry (Menarini Ricerche Sud, Pomezia, Italy) before pursuing a carrier in diagnostic pathology. He is a diplomate of the American Board of Pathology. He completed his residency training in Anatomical and Clinical Pathology at the Washington University School of Medicine, St. Louis, MO program (boarded in 2003), followed by a Fellowship in Hematopathology at the University of Pennsylvania (boarded in 2004). Arpad Szallasi is a past President for the New Jersey Association of Blood Bank Professional and a former medical advisor to the American Red Cross.

Affiliations and Expertise

MD PhD FCAP, Pathologist and Medical Director for the Transfusion Services, Monmouth Medical Center, Long Branch, NJ, Professor of Pathology and Laboratory Medicine, Drexel University College of Medicine, Philadelphia, PA and President, New Jersey Association of Blood Bank Professionals

Ratings and Reviews

Write a review

There are currently no reviews for "TRP Channels as Therapeutic Targets"