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Recent findings have implied a distinct therapeutic potential for drugs targeting Transient Receptor Potential (TRP) channels in a wide variety of diseases, many with no existing satisfactory treatment options. Thus, the TRP superfamily of ion channels has attracted a great deal of well-deserved attention. TRP Channels in Drug Discovery provides a thorough collection of the most up-to-date reviews and protocols on the subject, coming from top experts in the field. Volume I presents a series of state-of-the-art minireviews on the most interesting TRP channels (from TRPA1 to TRPV4), as well as TRP-related protocols involving airways and the genitourinary tract. Written for the Methods in Pharmacology and Toxicology(TM) series, this work includes the kind of detailed description and key implementation advice that ensures successful results in the lab.

Comprehensive and cutting-edge, TRP Channels in Drug Discovery serves as an ideal reference for graduate students in academic laboratories as well as for pharmaceutical scientists developing new drugs and clinicians interested in novel drugs in the pipeline.

TRP Channels in Drug Discovery: Volume I

Part I: Introduction

1. Introduction to TRPs: A Quest for Novel Drug Targets

Bernd Nilius

2. TRP-Mediated Cytoskeletal Reorganization: Implications for Disease and Drug Development

Chandan Goswami

Part II: TRP Channels, from A1 to V4

3. TRPA1 in Drug Discovery

Jun Chen, Steve McGaraughty, and Philip R. Kym

4. Canonical Transient Receptor Potential Channel (TRPC) Expression, Regulation, and Function in Vascular and Airway Diseases

Brij B. Singh, Christina M. Pabelick, and Y.S. Prakash

5. TRPM2 Function and Potential as a Drug Target

Barbara A. Miller

6. The Ca²⁺-Activated Monovalent Cation Selective Channels TRPM4 and TRPM5

Colsoul Barbara, Kecskes Miklos, Philippaert Koenraad, Menigoz Aurelie, and Vennekens Rudi

7. The Emerging Role of TRPM7 in the Regulation of Magnesium Homeostasis

Vladimir Chubanov, Jonathan T. Eggenschwiler, Thomas Gudermann, and Alexey G. Ryazanov

8. TRPM8 Channels as Potential Therapeutic Targets for Pain, Analgesia, and Thermoregulation

David D. McKemy

9. TRPML Channels in Function, Disease, and Prospective Therapies

David A. Zeevi

10. The TRPP Signalling Module: TRPP2/Polycystin 1 and TRPP2/PKD1L1

Alexis Hofherr

11. TRPV1 as a Polymodal Sensor: Potential to Discover TRPV1 Antagonists Selective for Specific Activating Modalities

Olivier Radresa, Stephen Zicha, William Brown, and Jennifer M.A. Laird

12. Nociceptive and Non-Nociceptive Roles of TRPV3 and Its "Druggability"

Sungjae Yoo and Sun Wook Hwang

13. TRPV4 and Drug Discovery

Fabien Vincent and Matthew A.J. Duncton

Part III: TRPs and Airways

14. TRP Expression and Function in the Lung Airways

Alexander Dietrich and Thomas Gudermann

15. Hypoxia-Dependent TRP Channel Function in Pulmonary Arterial Smooth Muscle Cells

Beate Fuchs, Hermann Kalwa, Norbert Weissmann, Thomas Gudermann, and Alexander Dietrich

16. Endotoxin-Induced Airway Inflammation and Asthma Models

Zsuzsanna Helyes and Zsófia Hajna

17. Enhanced Cough, Animal Models

Raffaele Gatti, Pamela Pedretti, Romina Nassini, and Marcello Trevisani

18. Capsaicin Inhalation Test in Man

Eva Millqvist

Part IV: TRPs and the Genitourinary (GU) Tract

19. TRP Channels in the Genitourinary (GU) Tract

Ana Charrua and Francisco Cruz

20. Animal Models of Cystitis

Célia D. Cruz and António Avelino

21. Overactive Bladder Models

Roberto Soler, Lysanne Campeau, Claudius Füllhase, and Karl-Erik Andersson

Alexis Hofherr

11. TRPV1 as a Polymodal Sensor: Potential to Discover TRPV1 Antagonists Selective for Specific Activating Modalities

Olivier Radresa, Stephen Zicha, William Brown, and Jennifer M.A. Laird

12. Nociceptive and Non-Nociceptive Roles of TRPV3 and Its "Druggability"

Sungjae Yoo and Sun Wook Hwang

13. TRPV4 and Drug Discovery

Fabien Vincent and Matthew A.J. Duncton

Part III: TRPs and Airways

14. TRP Expression and Function in the Lung Airways

Alexander Dietrich and Thomas Gudermann

15. Hypoxia-Dependent TRP Channel Function in Pulmonary Arterial Smooth Muscle Cells

Beate Fuchs, Hermann Kalwa, Norbert Weissmann, Thomas Gudermann, and Alexander Dietrich

16. Endotoxin-Induced Airway Inflammation and Asthma Models

Zsuzsanna Helyes and Zsófia Hajna

17. Enhanced Cough, Animal Models

Raffaele Gatti, Pamela Pedretti, Romina Nassini, and Marcello Trevisani

18. Capsaicin Inhalation Test in Man

Eva Millqvist

Part IV: TRPs and the Genitourinary (GU) Tract

19. TRP Channels in the Genitourinary (GU) Tract

Ana Charrua and Francisco Cruz

20. Animal Models of Cystitis

Célia D. Cruz and António Avelino

21. Overactive Bladder Models

Roberto Soler, Lysanne Campeau, Claudius Füllhase, and Karl-Erik Andersson

Olivier Radresa, Stephen Zicha, William Brown, and Jennifer M.A. Laird

12. Nociceptive and Non-Nociceptive Roles of TRPV3 and Its "Druggability"

Sungjae Yoo and Sun Wook Hwang

13. TRPV4 and Drug Discovery

Fabien Vincent and Matthew A.J. Duncton

Part III: TRPs and Airways

14. TRP Expression and Function in the Lung Airways

Alexander Dietrich and Thomas Gudermann

15. Hypoxia-Dependent TRP Channel Function in Pulmonary Arterial Smooth Muscle Cells

Beate Fuchs, Hermann Kalwa, Norbert Weissmann, Thomas Gudermann, and Alexander Dietrich

16. Endotoxin-Induced Airway Inflammation and Asthma Models

Zsuzsanna Helyes and Zsófia Hajna

17. Enhanced Cough, Animal Models

Raffaele Gatti, Pamela Pedretti, Romina Nassini, and Marcello Trevisani

18. Capsaicin Inhalation Test in Man

Eva Millqvist

Part IV: TRPs and the Genitourinary (GU) Tract

19. TRP Channels in the Genitourinary (GU) Tract

Ana Charrua and Francisco Cruz

20. Animal Models of Cystitis

Célia D. Cruz and António Avelino

21. Overactive Bladder Models

Roberto Soler, Lysanne Campeau, Claudius Füllhase, and Karl-Erik Andersson

Sungjae Yoo and Sun Wook Hwang

13. TRPV4 and Drug Discovery

Fabien Vincent and Matthew A.J. Duncton

Part III: TRPs and Airways

14. TRP Expression and Function in the Lung Airways

Alexander Dietrich and Thomas Gudermann

15. Hypoxia-Dependent TRP Channel Function in Pulmonary Arterial Smooth Muscle Cells

Beate Fuchs, Hermann Kalwa, Norbert Weissmann, Thomas Gudermann, and Alexander Dietrich

16. Endotoxin-Induced Airway Inflammation and Asthma Models

Zsuzsanna Helyes and Zsófia Hajna

17. Enhanced Cough, Animal Models

Raffaele Gatti, Pamela Pedretti, Romina Nassini, and Marcello Trevisani

18. Capsaicin Inhalation Test in Man

Eva Millqvist

Part IV: TRPs and the Genitourinary (GU) Tract

19. TRP Channels in the Genitourinary (GU) Tract

Ana Charrua and Francisco Cruz

20. Animal Models of Cystitis

Célia D. Cruz and António Avelino

21. Overactive Bladder Models

Roberto Soler, Lysanne Campeau, Claudius Füllhase, and Karl-Erik Andersson

Fabien Vincent and Matthew A.J. Duncton

Part III: TRPs and Airways

14. TRP Expression and Function in the Lung Airways

Alexander Dietrich and Thomas Gudermann

15. Hypoxia-Dependent TRP Channel Function in Pulmonary Arterial Smooth Muscle Cells

Beate Fuchs, Hermann Kalwa, Norbert Weissmann, Thomas Gudermann, and Alexander Dietrich

16. Endotoxin-Induced Airway Inflammation and Asthma Models

Zsuzsanna Helyes and Zsófia Hajna

17. Enhanced Cough, Animal Models

Raffaele Gatti, Pamela Pedretti, Romina Nassini, and Marcello Trevisani

18. Capsaicin Inhalation Test in Man

Eva Millqvist

Part IV: TRPs and the Genitourinary (GU) Tract

19. TRP Channels in the Genitourinary (GU) Tract

Ana Charrua and Francisco Cruz

20. Animal Models of Cystitis

Célia D. Cruz and António Avelino

21. Overactive Bladder Models

Roberto Soler, Lysanne Campeau, Claudius Füllhase, and Karl-Erik Andersson

Raffaele Gatti, Pamela Pedretti, Romina Nassini, and Marcello Trevisani

18. Capsaicin Inhalation Test in Man

Eva Millqvist

Part IV: TRPs and the Genitourinary (GU) Tract

19. TRP Channels in the Genitourinary (GU) Tract

Ana Charrua and Francisco Cruz

20. Animal Models of Cystitis

Célia D. Cruz and António Avelino

21. Overactive Bladder Models

Roberto Soler, Lysanne Campeau, Claudius Füllhase, and Karl-Erik Andersson

Eva Millqvist

Part IV: TRPs and the Genitourinary (GU) Tract

19. TRP Channels in the Genitourinary (GU) Tract

Ana Charrua and Francisco Cruz

20. Animal Models of Cystitis

Célia D. Cruz and António Avelino

21. Overactive Bladder Models

Roberto Soler, Lysanne Campeau, Claudius Füllhase, and Karl-Erik Andersson

19. TRP Channels in the Genitourinary (GU) Tract

Ana Charrua and Francisco Cruz

20. Animal Models of Cystitis

Célia D. Cruz and António Avelino

21. Overactive Bladder Models

Roberto Soler, Lysanne Campeau, Claudius Füllhase, and Karl-Erik Andersson

Ana Charrua and Francisco Cruz

20. Animal Models of Cystitis

Célia D. Cruz and António Avelino

21. Overactive Bladder Models

Roberto Soler, Lysanne Campeau, Claudius Füllhase, and Karl-Erik Andersson

Roberto Soler, Lysanne Campeau, Claudius Füllhase, and Karl-Erik Andersson