Annual Reports in Medicinal Chemistry, Volume 46

1st Edition

Series Editors: John Macor
Paperback ISBN: 9780123860095
eBook ISBN: 9780123860248
Imprint: Academic Press
Published Date: 24th October 2011
Page Count: 624
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Table of Contents



Chapter 1: Progress in the Medicinal Chemistry of Group III Metabotropic Glutamate Receptors

1. Introduction

2. Group III Orthosteric Ligands

3. mGlu4 Receptor Allosteric Ligands

4. mGlu6 Receptor Ligands

5. mGlu7 Receptor Ligands

6. mGlu8 Receptor Ligands

7. Conclusions

Chapter 2: Recent Advances Toward Pain Therapeutics

1. Introduction

2. Sodium Channel Blockers

3. NGF/TrkA Pathway Interference

4. FAAH Inhibitors

5. Conclusions

Chapter 3: Central Modulation of Circadian Rhythm via CK1 Inhibition for Psychiatric Indications

1. Introduction

2. Description of Circadian Clock

3. CK1 Inhibitors

4. Preclinical Animal Models

5. Conclusions

Chapter 4: Recent Progress in the Discovery of Kv7 Modulators

1. Introduction

2. Kv7.1 Channels

3. Kv7.2–Kv7.5 Channels

4. Conclusion

Chapter 5: Bile Acid Receptor Modulators in Metabolic Diseases

1. Introduction

2. FXR Agonists

3. TGR5 Agonists

4. FXR/TGR5 Dual Agonists

5. Clinical Studies and Outlook

Chapter 6: Recent Advances in Mineralocorticoid Receptor Antagonists

1. Introduction

2. Aldosterone and MR Biology

3. RAAS Pathway, MR Antagonists versus ACE, ARB Therapy

4. Structural Features of the Ligand Binding Domain of MR

5. Current Medicinal Chemistry Efforts

6. Conclusions

Chapter 7: SGLT2 Inhibitors for Type 2 Diabetes

1. Introduction

2. SGLT2 Physiology

3. Clinical Trials

4. SGLT2 Inhibitors

5. Conclusion

Chapter 8: Recent Advances in the Discovery and Development of CRTh2 Antagonists

1. Introduction

2. CRTh2 Antagonists

3. Conclusions

Chapter 9: Developments and Advances in Gastrointestinal Prokinetic


Annual Reports in Medicinal Chemistry provides timely and critical reviews of important topics in medicinal chemistry together with an emphasis on emerging topics in the biological sciences, which are expected to provide the basis for entirely new future therapies.


medicinal, pharmaceutical, and organic chemists


No. of pages:
© Academic Press 2011
Academic Press
eBook ISBN:
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This series is one of the very few annual publications which justify the title of an absolute must for the pharmacologist, chemist, or physician who is interested in the chemistry of drug development." - ENZYMOLOGIA

About the Series Editors

John Macor Series Editor

Affiliations and Expertise

Neuroscience Discovery Chemistry, Bristol-Myers Squibb, USA