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Blood-brain barrier in drug discovery : optimizing brain exposure of CNS drugs and minimizing brain side effects for peripheral drugs / / edited by Li Di, Edward H. Kerns
| Blood-brain barrier in drug discovery : optimizing brain exposure of CNS drugs and minimizing brain side effects for peripheral drugs / / edited by Li Di, Edward H. Kerns |
| Edizione | [1st ed.] |
| Pubbl/distr/stampa | Hoboken, New Jersey : , : John Wiley & Sons Inc., , [2015] |
| Descrizione fisica | 1 online resource (607 p.) |
| Disciplina | 615.7/8 |
| Soggetto topico |
Brain - Effect of drugs on
Blood-brain barrier |
| ISBN |
1-118-78852-4
1-118-78854-0 |
| Formato | Materiale a stampa  |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Nota di contenuto | Machine generated contents note: Summary List of Chapters1. Overview/Introduction / Li Di (Pfizer Inc.), Edward H. Kerns (Pharmacokinetics of Brain Exposure)2. Pharmacokinetics of CNS penetration / Andreas Reichel (Bayer)3. Free Drug Hyposthesis for CNS Drug Candidates / Xingrong Liu (Genentech)4. Species Differences and impact of desease state on BBB / Jean-Marie Nicolas (UCB Pharma S.A.)Mechanisms of Drugs Across the Blood-Brain Barrier5. Passive diffusion permeability of the BBB - examples and SAR / Phil Jeffrey (GSK)6. Efflux transport at the BBB - examples and SAR / Jerome Hochman (Merck)7. Uptake transport at the BBB - examples and SAR / Zack Cheng (AstraZeneca)8. Uptake of proteins and antibodies at the BBB / William Pardridge (UCLA)Predicting and Measuring Brain Exposure of Drugs9. In silico tools for assessing brain exposure / Hongming Chen (AstraZeneca)10. In vitro assays for assessing BBB permeability - vascular cells, artificial membranes, brain slice, cell uptake / Winfried Neuhaus (University of Vienna)11. Human-based in vitro endothelial cell models / Eric Shusta (University of Wisconsin)12. In vitro assays for assessing brain binding / Li Di (Pfizer)13. In vivo studies of brain exposure / Edward H. Kerns14. PBPK models for BBB / Elizabeth de Lange (Leiden University)15. PK/PD modeling of CNS drug candidates / Johan Gabrielsson (Swedish University)16. Microdialysis to assess free drug concentration in brain / William Kielbasa (Lilly)17. Imaging technique for CNS drug discovery / Lei Zhang (Pfizer Inc.)Modulating Brain Penetration of Leads During Drug Discovery18. Designing CNS drugs for optimal brain exposure / Zoran Rankovic (Lilly)19. Case studies of CNS drug optimization - medicinal chemistry and CNS biology perspectives / Kevin J. Hodgetts (Harvard NeuroDiscovery Center)20. Designing peripheral drugs for minimal brain exposue / Peter Bungay (Pfizer)21. Case studies of non-CNS drugs to minimize brain penetration - Nonsudative antihistamines / Andrew Crowe (Curtin University)Case Studies in CNS Drug Discovery22. Case study 1 on discovery of a successful CNS drug - Fycompa (AMPA Receptor Antagonist) / Andrew Satlin and Antonio Laurenza (Eisai)23. Case study 2 on discovery of a successful CNS drug - Vortioxetine (Serotonin Modulator and Stimulator) / Benny Bang-Andersen (Lundbeck)Drug Delivery Techniques to CNS24. Brain delivery using nanotechnology / Xinguo Jiang (Fudan University)25. Intranasal delivery to CNS / Lisbeth Illum (University of Nottingham)Future Prospective in Blood Brain Barrier Advancement26. Conclusion Remarks / Joan Abbott (King's College). |
| Record Nr. | UNINA-9910132304003321 |
| Hoboken, New Jersey : , : John Wiley & Sons Inc., , [2015] | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
Blood-brain barrier in drug discovery : optimizing brain exposure of CNS drugs and minimizing brain side effects for peripheral drugs / / edited by Li Di, Edward H. Kerns
| Blood-brain barrier in drug discovery : optimizing brain exposure of CNS drugs and minimizing brain side effects for peripheral drugs / / edited by Li Di, Edward H. Kerns |
| Edizione | [1st ed.] |
| Pubbl/distr/stampa | Hoboken, New Jersey : , : John Wiley & Sons Inc., , [2015] |
| Descrizione fisica | 1 online resource (607 p.) |
| Disciplina | 615.7/8 |
| Soggetto topico |
Brain - Effect of drugs on
Blood-brain barrier |
| ISBN |
1-118-78852-4
1-118-78854-0 |
| Formato | Materiale a stampa |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Nota di contenuto | Machine generated contents note: Summary List of Chapters1. Overview/Introduction / Li Di (Pfizer Inc.), Edward H. Kerns (Pharmacokinetics of Brain Exposure)2. Pharmacokinetics of CNS penetration / Andreas Reichel (Bayer)3. Free Drug Hyposthesis for CNS Drug Candidates / Xingrong Liu (Genentech)4. Species Differences and impact of desease state on BBB / Jean-Marie Nicolas (UCB Pharma S.A.)Mechanisms of Drugs Across the Blood-Brain Barrier5. Passive diffusion permeability of the BBB - examples and SAR / Phil Jeffrey (GSK)6. Efflux transport at the BBB - examples and SAR / Jerome Hochman (Merck)7. Uptake transport at the BBB - examples and SAR / Zack Cheng (AstraZeneca)8. Uptake of proteins and antibodies at the BBB / William Pardridge (UCLA)Predicting and Measuring Brain Exposure of Drugs9. In silico tools for assessing brain exposure / Hongming Chen (AstraZeneca)10. In vitro assays for assessing BBB permeability - vascular cells, artificial membranes, brain slice, cell uptake / Winfried Neuhaus (University of Vienna)11. Human-based in vitro endothelial cell models / Eric Shusta (University of Wisconsin)12. In vitro assays for assessing brain binding / Li Di (Pfizer)13. In vivo studies of brain exposure / Edward H. Kerns14. PBPK models for BBB / Elizabeth de Lange (Leiden University)15. PK/PD modeling of CNS drug candidates / Johan Gabrielsson (Swedish University)16. Microdialysis to assess free drug concentration in brain / William Kielbasa (Lilly)17. Imaging technique for CNS drug discovery / Lei Zhang (Pfizer Inc.)Modulating Brain Penetration of Leads During Drug Discovery18. Designing CNS drugs for optimal brain exposure / Zoran Rankovic (Lilly)19. Case studies of CNS drug optimization - medicinal chemistry and CNS biology perspectives / Kevin J. Hodgetts (Harvard NeuroDiscovery Center)20. Designing peripheral drugs for minimal brain exposue / Peter Bungay (Pfizer)21. Case studies of non-CNS drugs to minimize brain penetration - Nonsudative antihistamines / Andrew Crowe (Curtin University)Case Studies in CNS Drug Discovery22. Case study 1 on discovery of a successful CNS drug - Fycompa (AMPA Receptor Antagonist) / Andrew Satlin and Antonio Laurenza (Eisai)23. Case study 2 on discovery of a successful CNS drug - Vortioxetine (Serotonin Modulator and Stimulator) / Benny Bang-Andersen (Lundbeck)Drug Delivery Techniques to CNS24. Brain delivery using nanotechnology / Xinguo Jiang (Fudan University)25. Intranasal delivery to CNS / Lisbeth Illum (University of Nottingham)Future Prospective in Blood Brain Barrier Advancement26. Conclusion Remarks / Joan Abbott (King's College). |
| Record Nr. | UNINA-9910829110403321 |
| Hoboken, New Jersey : , : John Wiley & Sons Inc., , [2015] | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
Drug-like properties [[electronic resource] ] : concepts, structure design and methods : from ADME to toxicity optimization / / Edward H. Kerns and Li Di
| Drug-like properties [[electronic resource] ] : concepts, structure design and methods : from ADME to toxicity optimization / / Edward H. Kerns and Li Di |
| Autore | Kerns Edward Harvel |
| Pubbl/distr/stampa | Amsterdam ; ; Boston, : Academic Press, c2008 |
| Descrizione fisica | 1 online resource (549 p.) |
| Disciplina | 615/.19 |
| Altri autori (Persone) | DiLi |
| Soggetto topico |
Pharmaceutical chemistry
Drugs - Structure-activity relationships Drug development Drugs - Design |
| Soggetto genere / forma | Electronic books. |
| ISBN |
1-281-76371-3
9786611763718 0-08-095162-7 0-08-055761-9 |
| Formato | Materiale a stampa |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Nota di contenuto |
Front Cover; Drug-like Properties: Concepts, Structure Design and Methods: from ADME to Toxicity Optimization; Copyright Page; Table of Contents; Preface; Dedication; Part 1 Introductory Concepts; Chapter 1 Introduction; Problems; References; Chapter 2 Advantages of Good Drug-like Properties; 2.1 Drug-like Properties Are an Integral Part of Drug Discovery; 2.1.1 Many Properties Are of Interest in Discovery; 2.1.2 Introduction to the Drug Discovery and Development Process; 2.1.3 Development Attrition is Reduced by Improving Drug Properties
2.1.4 Poor Drug Properties Also Cause Discovery Inefficiencies2.1.5 Marginal Drug Properties Cause Inefficiencies During Development; 2.1.6 Poor Properties Can Cause Poor Discovery Research; 2.2 Changing Emphasis on Properties in Discovery; 2.3 Property Profiling in Discovery; 2.4 Drug-like Property Optimization in Discovery; Problems; References; Chapter 3 Barriers to Drug Exposure in Living Systems; 3.1 Introduction to Barriers; 3.2 Drug Dosing; 3.3 Barriers in the Mouth and Stomach; 3.4 Gastrointestinal Tract Barriers; 3.4.1 Permeation of the Gastrointestinal Cellular Membrane 3.4.2 Passive Diffusion at the Molecular Level3.4.3 Metabolism in the Intestine; 3.4.4 Enzymatic Hydrolysis in the Intestine; 3.4.5 Absorption Enhancement in the Intestine; 3.5 Barriers in the Bloodstream; 3.5.1 Plasma Enzyme Hydrolysis; 3.5.2 Plasma Protein Binding; 3.5.3 Red Blood Cell Binding; 3.6 Barriers in the Liver; 3.6.1 Metabolism; 3.6.2 Biliary Excretion; 3.7 Barriers in the Kidney; 3.8 Blood-Tissue Barriers; 3.9 Tissue Distribution; 3.10 Consequences of Chirality on Barriers and Properties; 3.11 Overview of In Vivo Barriers; Problems; References; Part 2 Physicochemical Properties Chapter 4 Rules for Rapid Property Profiling from Structure4.1 Lipinski Rules; 4.2 Veber Rules; 4.3 Other Rules; 4.4 Application of Rules for Compound Assessment; Problems; References; Chapter 5 Lipophilicity; 5.1 Lipophilicity Fundamentals; 5.2 Lipophilicity Effects; 5.3 Lipophilicity Case Studies and Structure Modification; Problems; References; Chapter 6 pKa; 6.1 pKa Fundamentals; 6.2 pKa Effects; 6.3 pKa Case Studies; 6.4 Structure Modification Strategies for pKa; Problems; References; Chapter 7 Solubility; 7.1 Solubility Fundamentals 7.1.1 Solubility Varies with Structure and Physical Conditions7.1.2 Dissolution Rate; 7.1.3 Structural Properties Affect Solubility; 7.1.4 Kinetic and Thermodynamic Solubility; 7.2 Effects of Solubility; 7.2.1 Low Solubility Limits Absorption and Causes Low Oral Bioavailability; 7.2.2 Good Solubility is Essential for IV Formulation; 7.2.3 Acceptance Criteria and Classifications for Solubility; 7.2.4 Molecular Properties for Solubility and Permeability Often are Opposed; 7.3 Effects of Physiology on Solubility and Absorption; 7.3.1 Physiology of the Gastrointestinal Tract 7.3.2 Species Differences in Gastrointestinal Tract |
| Record Nr. | UNINA-9910453434903321 |
Kerns Edward Harvel
|
||
| Amsterdam ; ; Boston, : Academic Press, c2008 | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
Drug-like properties : concepts, structure design and methods : from ADME to toxicity optimization / / Edward H. Kerns and Li Di
| Drug-like properties : concepts, structure design and methods : from ADME to toxicity optimization / / Edward H. Kerns and Li Di |
| Autore | Kerns Edward Harvel |
| Pubbl/distr/stampa | Amsterdam ; ; Boston : , : Academic Press, , 2008 |
| Descrizione fisica | 1 online resource (xix, 526 pages, 2 unnumbered pages of plates) : illustrations (some color) |
| Disciplina | 615/.19 |
| Altri autori (Persone) | DiLi |
| Soggetto topico |
Pharmaceutical chemistry
Drugs - Structure-activity relationships Drug development Drugs - Design |
| ISBN |
1-281-76371-3
9786611763718 0-08-095162-7 0-08-055761-9 |
| Formato | Materiale a stampa |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Nota di contenuto |
Front Cover; Drug-like Properties: Concepts, Structure Design and Methods: from ADME to Toxicity Optimization; Copyright Page; Table of Contents; Preface; Dedication; Part 1 Introductory Concepts; Chapter 1 Introduction; Problems; References; Chapter 2 Advantages of Good Drug-like Properties; 2.1 Drug-like Properties Are an Integral Part of Drug Discovery; 2.1.1 Many Properties Are of Interest in Discovery; 2.1.2 Introduction to the Drug Discovery and Development Process; 2.1.3 Development Attrition is Reduced by Improving Drug Properties
2.1.4 Poor Drug Properties Also Cause Discovery Inefficiencies; 2.1.5 Marginal Drug Properties Cause Inefficiencies During Development; 2.1.6 Poor Properties Can Cause Poor Discovery Research; 2.2 Changing Emphasis on Properties in Discovery; 2.3 Property Profiling in Discovery; 2.4 Drug-like Property Optimization in Discovery; Problems; References; Chapter 3 Barriers to Drug Exposure in Living Systems; 3.1 Introduction to Barriers; 3.2 Drug Dosing; 3.3 Barriers in the Mouth and Stomach; 3.4 Gastrointestinal Tract Barriers; 3.4.1 Permeation of the Gastrointestinal Cellular Membrane 3.4.2 Passive Diffusion at the Molecular Level; 3.4.3 Metabolism in the Intestine; 3.4.4 Enzymatic Hydrolysis in the Intestine; 3.4.5 Absorption Enhancement in the Intestine; 3.5 Barriers in the Bloodstream; 3.5.1 Plasma Enzyme Hydrolysis; 3.5.2 Plasma Protein Binding; 3.5.3 Red Blood Cell Binding; 3.6 Barriers in the Liver; 3.6.1 Metabolism; 3.6.2 Biliary Excretion; 3.7 Barriers in the Kidney; 3.8 Blood-Tissue Barriers; 3.9 Tissue Distribution; 3.10 Consequences of Chirality on Barriers and Properties; 3.11 Overview of In Vivo Barriers; Problems; References; Part 2 Physicochemical Properties Chapter 4 Rules for Rapid Property Profiling from Structure; 4.1 Lipinski Rules; 4.2 Veber Rules; 4.3 Other Rules; 4.4 Application of Rules for Compound Assessment; Problems; References; Chapter 5 Lipophilicity; 5.1 Lipophilicity Fundamentals; 5.2 Lipophilicity Effects; 5.3 Lipophilicity Case Studies and Structure Modification; Problems; References; Chapter 6 pKa; 6.1 pKa Fundamentals; 6.2 pKa Effects; 6.3 pKa Case Studies; 6.4 Structure Modification Strategies for pKa; Problems; References; Chapter 7 Solubility; 7.1 Solubility Fundamentals 7.1.1 Solubility Varies with Structure and Physical Conditions; 7.1.2 Dissolution Rate; 7.1.3 Structural Properties Affect Solubility; 7.1.4 Kinetic and Thermodynamic Solubility; 7.2 Effects of Solubility; 7.2.1 Low Solubility Limits Absorption and Causes Low Oral Bioavailability; 7.2.2 Good Solubility is Essential for IV Formulation; 7.2.3 Acceptance Criteria and Classifications for Solubility; 7.2.4 Molecular Properties for Solubility and Permeability Often are Opposed; 7.3 Effects of Physiology on Solubility and Absorption; 7.3.1 Physiology of the Gastrointestinal Tract; 7.3.2 Species Differences in Gastrointestinal Tract |
| Record Nr. | UNINA-9910782360503321 |
|
Kerns Edward Harvel
|
||
| Amsterdam ; ; Boston : , : Academic Press, , 2008 | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
Drug-like properties : concepts, structure design and methods : from ADME to toxicity optimization / / Edward H. Kerns and Li Di
| Drug-like properties : concepts, structure design and methods : from ADME to toxicity optimization / / Edward H. Kerns and Li Di |
| Autore | Kerns Edward Harvel |
| Edizione | [1st ed.] |
| Pubbl/distr/stampa | Amsterdam ; ; Boston, : Academic Press, c2008 |
| Descrizione fisica | 1 online resource (xix, 526 pages, 2 unnumbered pages of plates) : illustrations (some color) |
| Disciplina | 615/.19 |
| Altri autori (Persone) | DiLi |
| Soggetto topico |
Pharmaceutical chemistry
Drugs - Structure-activity relationships Drug development Drugs - Design |
| ISBN |
1-281-76371-3
9786611763718 0-08-095162-7 0-08-055761-9 |
| Formato | Materiale a stampa |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Nota di contenuto |
Front Cover; Drug-like Properties: Concepts, Structure Design and Methods: from ADME to Toxicity Optimization; Copyright Page; Table of Contents; Preface; Dedication; Part 1 Introductory Concepts; Chapter 1 Introduction; Problems; References; Chapter 2 Advantages of Good Drug-like Properties; 2.1 Drug-like Properties Are an Integral Part of Drug Discovery; 2.1.1 Many Properties Are of Interest in Discovery; 2.1.2 Introduction to the Drug Discovery and Development Process; 2.1.3 Development Attrition is Reduced by Improving Drug Properties
2.1.4 Poor Drug Properties Also Cause Discovery Inefficiencies; 2.1.5 Marginal Drug Properties Cause Inefficiencies During Development; 2.1.6 Poor Properties Can Cause Poor Discovery Research; 2.2 Changing Emphasis on Properties in Discovery; 2.3 Property Profiling in Discovery; 2.4 Drug-like Property Optimization in Discovery; Problems; References; Chapter 3 Barriers to Drug Exposure in Living Systems; 3.1 Introduction to Barriers; 3.2 Drug Dosing; 3.3 Barriers in the Mouth and Stomach; 3.4 Gastrointestinal Tract Barriers; 3.4.1 Permeation of the Gastrointestinal Cellular Membrane 3.4.2 Passive Diffusion at the Molecular Level; 3.4.3 Metabolism in the Intestine; 3.4.4 Enzymatic Hydrolysis in the Intestine; 3.4.5 Absorption Enhancement in the Intestine; 3.5 Barriers in the Bloodstream; 3.5.1 Plasma Enzyme Hydrolysis; 3.5.2 Plasma Protein Binding; 3.5.3 Red Blood Cell Binding; 3.6 Barriers in the Liver; 3.6.1 Metabolism; 3.6.2 Biliary Excretion; 3.7 Barriers in the Kidney; 3.8 Blood-Tissue Barriers; 3.9 Tissue Distribution; 3.10 Consequences of Chirality on Barriers and Properties; 3.11 Overview of In Vivo Barriers; Problems; References; Part 2 Physicochemical Properties Chapter 4 Rules for Rapid Property Profiling from Structure; 4.1 Lipinski Rules; 4.2 Veber Rules; 4.3 Other Rules; 4.4 Application of Rules for Compound Assessment; Problems; References; Chapter 5 Lipophilicity; 5.1 Lipophilicity Fundamentals; 5.2 Lipophilicity Effects; 5.3 Lipophilicity Case Studies and Structure Modification; Problems; References; Chapter 6 pKa; 6.1 pKa Fundamentals; 6.2 pKa Effects; 6.3 pKa Case Studies; 6.4 Structure Modification Strategies for pKa; Problems; References; Chapter 7 Solubility; 7.1 Solubility Fundamentals 7.1.1 Solubility Varies with Structure and Physical Conditions; 7.1.2 Dissolution Rate; 7.1.3 Structural Properties Affect Solubility; 7.1.4 Kinetic and Thermodynamic Solubility; 7.2 Effects of Solubility; 7.2.1 Low Solubility Limits Absorption and Causes Low Oral Bioavailability; 7.2.2 Good Solubility is Essential for IV Formulation; 7.2.3 Acceptance Criteria and Classifications for Solubility; 7.2.4 Molecular Properties for Solubility and Permeability Often are Opposed; 7.3 Effects of Physiology on Solubility and Absorption; 7.3.1 Physiology of the Gastrointestinal Tract; 7.3.2 Species Differences in Gastrointestinal Tract |
| Record Nr. | UNINA-9910827925703321 |
|
Kerns Edward Harvel
|
||
| Amsterdam ; ; Boston, : Academic Press, c2008 | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||