Drug Discovery and Development [Paperback]

Overview.- Drug Discovery and Development: Reflections and Projections.- 1. Introduction.- 2. Drug Discovery.- 2.1. General Issues.- 2.2. Compound Sources.- 2.3. Goal Identification.- 3. The Project Team.- 4. The Flow Chart.- 4.1. The Primary Screen.- 4.2. The Secondary Screen.- 4.3. The Tertiary Screen.- 4.4. Networking.- 4.5. Backup Compounds.- 5. Toxicological Evaluation.- 6. Clinical Evaluation.- 7. Newer Aspects Of Drug Development.- 7.1. The Mechanistic Approach.- 7.2. Drug Delivery.- 8. The Future.- 8.1. The Industry.- 8.2. & and Society.- References.- Compound Discovery.- Drug Design.- 1. Drug Design.- 2. Lead Discovery by Design.- 3. Lead Discovery by Random and Directed Screening.- 4. Quantitative Structure-Activity Relationships.- 5. Pattern Recognition.- 6. Lead Development.- 6.1. Systematic Empirical Approach.- 6.2. Hypothesis-Based Lead Development.- 7. Conclusion.- References.- Computer-Based Approaches to Drug Design.- 1. Introduction.- 2. Theoretical Calculations.- 2.1. Molecular Mechanics-Based Approaches.- 2.2. General Limitations of Theoretical Calculations.- 2.3. Quantum Mechanics-Based Approaches.- 3. Graphical Displays of Molecular Geometry and Steric Volume.- 4. Display of Electronic Properties.- 4.1. Limitations of Partial Charges in Modeling Electronic Interactions.- 4.2. Electrostatic Potential Displays.- 4.3. Qualitative Nature of Electrostatic Potential Displays.- 4.4 Isopotential Surface Displays.- 5. Macromolecular Systems.- References.- Use of Intact Tissue Preparations in the Drug Discovery Process.- 1. Introduction.- 2. General Concepts.- 2.1. Receptors.- 2.2. Dose-Response.- 3. Relevance to Drug Development.- 3.1. Calcium Antagonists.- 3.2. H2 Antagonists.- 3.3. Leukotriene Antagonists.- 4. Summary.- References.- Neuropsychopharmacological Drug Development.- 1. Introduction.- 2. Anxiolytic Drug Discovery and Development.- 2.1. Antianxiety Activity.- 2.2. Anticonvulsant Activity.- 2.3. Muscle Relaxant Potential.- 2.4. Assessment of l“$