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Informationen zum Autor Richard Glennon is Chair of the Department of Medicinal Chemistry at Virginia Commonwealth University. He is the author of over four hundred scientific publications and book chapters. Richard Young is an Associate Professor in the Department of Medicinal Chemistry at Virginia Commonwealth University. Previously, he worked in the pharmaceutical industry at Ayerst and A. H. Robins (both now Pfizer). Klappentext Drug discrimination: a practical guide to its contributions to the invention of new chemical entities and evaluations of new or known pharmacological agentsDrug discrimination can be described as a "drug detection" procedure that uses a pharmacologically active agent as the subjective stimulus. Although the procedure does require some effort to implement, it can be an extremely important tool for understanding drug action. Whereas medicinal chemists should come to learn the types of information that drug discrimination studies can offer, pharmacologists and psychologists might come to realize how medicinal chemists can apply the types of information that the paradigm routinely provides. Drug Discrimination: Applications to Medicinal Chemistry and Drug Studies provides in-depth analyses of the nature and use of drugs as discriminative stimuli and bridges some of the numerous gaps between medicinal chemistry, pharmacology, and psychology.Stressing the practical aspects of drug discrimination, including types of procedures, study design, data, and interpretation, the book details the advantages and limitations of drug discrimination studies versus other pharmacologic evaluations. Practical information from leading researchers in the field addresses specific topics and techniques that are of interest in drug discovery, evaluation, and development.A groundbreaking new guide to the applications of drug discrimination studies for medicinal chemistry and neuroscience, Drug Discrimination is essential for any scientist, researcher, or student whose interests involve the design, development, and/or action of drugs acting at the level of the central nervous system. Zusammenfassung Although somewhat labor intensive, Drug Discrimination (DD) is of enormous applicability to the understanding of drug action. Inhaltsverzeichnis Preface xv Contributors xix Part I 1 Richard A. Glennon and Richard Young 1. An Introduction to Drug Discrimination 3 A. General Scope and Introductory Comments 3 B. Background and Utility of the Drug Discrimination Paradigm 7 C. Drug Discrimination: A Synopsis of the Approach 10 D. Drug Discrimination and Drugs of Abuse 11 E. Advantage of the Drug Discrimination Procedure 14 2. Methodological Considerations 19 A. Apparatus 19 B. Subjects 22 C. Operant Conditioning 23 3. Drug Discrimination: Practical Considerations 41 A. Drugs as Discriminative Stimuli 42 B. Choice of Dose and Pre-session Injection Interval 49 C. Discrimination Training Procedure 51 D. Discrimination Data 52 E. Testing 60 F. Data Analysis and Interpretations 78 G. Selected Topics 99 4. Role of Stereochemistry in Drug Discrimination Studies 129 A. Structural Isomers: Introduction 129 B. Constitutional Isomers 130 C. Stereoisomers 136 5. Drug Discrimination and in Vivo Structure-Activity Relationships 163 A. Structure-Activity Caveats 163 B. Phenylalkylamines Hallucinogens and Stimulants 165 C. Benzodiazepines 175 D. Neuronal Nicotinic Acetylcholinergic receptor Agents 177 E. Aminotetralins 178 6. Drug Discrimination and Mechanisms of Drug Action 183 A. Early Considerations 184 B. Classical Hallucinogens 186 C. Amphetamine-Related Stimulants 192 D. ...