TRP Channels as Therapeutic Targets

From Basic Science to Clinical Use

1st Edition - March 14, 2015
Editor: Arpad Szallasi
Language: English
Hardback ISBN:
9 7 8 - 0 - 1 2 - 4 2 0 0 2 4 - 1
eBook ISBN:
9 7 8 - 0 - 1 2 - 4 2 0 0 7 9 - 1

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 thera… Read more

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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.

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

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TRP Channels as Therapeutic Targets

From Basic Science to Clinical Use

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Save 50% on book bundles

Institutional subscription on ScienceDirect

Arpad Szallasi