| Description |
1 online resource (xvii, 573 pages) : illustrations. |
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text txt rdacontent |
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computer c rdamedia |
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online resource cr rdacarrier |
| Series |
Annual reports in medicinal chemistry ; v. 46
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| Note |
"Sponsored by the Division of Medicinal Chemistry of the American Chemical Society." |
| Bibliography |
Includes bibliographical references and index. |
| Note |
Print version record. |
| Contents |
Front Matter; Annual Reports in Medicinal Chemistry; Copyright; Contents; Contributors; Preface; Part I:: Central Nervous System Diseases; Chapter 1: Progress in the Medicinal Chemistry of Group III Metabotropic Glutamate Receptors; 1. Introduction; 2. Group III Orthosteric Ligands; 2.1. Group III agonists; 2.2. Group III antagonists; 3. mGlu4 Receptor Allosteric Ligands; 3.1. mGlu4 receptor positive allosteric modulators; 3.2. mGlu4 receptor negative allosteric modulators; 4. mGlu6 Receptor Ligands; 5. mGlu7 Receptor Ligands; 6. mGlu8 Receptor Ligands; 7. Conclusions; References |
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Chapter 2: Recent Advances Toward Pain Therapeutics1. Introduction; 2. Sodium Channel Blockers; 2.1. Nav subtypes as pain targets; 2.2. Pharmacological versus functional selectivity via state-dependent inhibition; 2.3. Subtype-selective inhibitors; 3. NGF/TrkA Pathway Interference; 3.1. NGF sequestration; 3.2. Inhibition of NGF/TrkA interaction; 3.3. TrkA kinase inhibitors; 4. FAAH Inhibitors; 4.1. Covalent FAAH inhibitors; 4.2. Noncovalent FAAH inhibitors; 5. Conclusions; References; Chapter 3: Central Modulation of Circadian Rhythm via CK1 Inhibition for Psychiatric Indications |
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1. Introduction2. Description of Circadian Clock; 3. CK1 Inhibitors; 3.1. Structure and function of CK1 enzymes; 3.2. Mechanism of action of CK1 inhibitors; 3.3. CK1 inhibitor chemical scaffolds; 4. Preclinical Animal Models; 5. Conclusions; References; Chapter 4: Recent Progress in the Discovery of Kv7 Modulators; 1. Introduction; 1.1. Function; 1.2. Structural biology; 2. Kv7.1 Channels; 3. Kv7.2-Kv7.5 Channels; 3.1. Function; 3.2. Binding sites; 3.3. Compounds in clinical development: Flupirtine, retigabine, and ICA105665; 3.4. Compounds in drug discovery |
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3.4.1. Efforts using retigabine/flupirtine as template3.4.2. Other Kv7 activators; 4. Conclusion; References; Part II:: Cardiovascular and Metabolic Diseases; Chapter 5: Bile Acid Receptor Modulators in Metabolic Diseases; 1. Introduction; 2. FXR Agonists; 3. TGR5 Agonists; 3.1. Non-BA agonists; 3.2. BA derivatives; 4. FXR/TGR5 Dual Agonists; 5. Clinical Studies and Outlook; References; Chapter 6: Recent Advances in Mineralocorticoid Receptor Antagonists; 1. Introduction; 2. Aldosterone and MR Biology; 3. RAAS Pathway, MR Antagonists versus ACE, ARB Therapy |
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3.1. Steroid-based MR antagonists in the clinic-Clinical results4. Structural Features of the Ligand Binding Domain of MR; 5. Current Medicinal Chemistry Efforts; 5.1. Dihydropyridines; 5.2. Pyrazoline derivatives; 5.3. Indole sulfonamides and related structures; 5.4. Benzimidazole derivatives; 5.5. Other MR antagonist structures; 6. Conclusions; References; Chapter 7: SGLT2 Inhibitors for Type 2 Diabetes; 1. Introduction; 2. SGLT2 Physiology; 2.1. Renal glucose reuptake by SGLT2 and SGLT1; 2.2. Glucosuria and regulation of plasma glucose; 3. Clinical Trials; 4. SGLT2 Inhibitors |
| Summary |
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. |
| Language |
English. |
| Subject |
Pharmaceutical chemistry.
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Clinical chemistry.
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Chemistry, Pharmaceutical |
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Chemistry, Clinical |
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Chimie pharmaceutique.
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Chimie clinique.
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MEDICAL -- Drug Guides.
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MEDICAL -- Nursing -- Pharmacology.
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MEDICAL -- Pharmacology.
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MEDICAL -- Pharmacy.
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Clinical chemistry
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Pharmaceutical chemistry
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| Added Author |
Macor, John Eugene.
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American Chemical Society. Division of Medicinal Chemistry.
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| ISBN |
9780123860248 (electronic bk.) |
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0123860245 (electronic bk.) |
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9780123860095 |
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1283299003 |
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9781283299008 |
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9786613299000 |
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6613299006 |
| Standard No. |
AU@ 000051596239 |
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