Not much more than a decade has passed since the appearance of the outstanding handbook, Catecholamines, edited by BLASCHKO and MUSCHOLL, in the series: Handbook of Experimental Pharmacology. However, this extremely well organized volume dealt mainly with the origin, molecular actions, and fate of the naturally occuring catecholamines. It was felt that a separate volume should be dedicated to the remarkable and exciting progress made in the field of agents influencing the adrenergic system, both in physiologic and pharmacologic respect. The editor of the present volume considers himself lucky to have been able to persuade a number of eminent specialists to collaborate. The main concept of the present handbook is a systematic approach to the various effects of adrenergic activators and inhibitors starting with the chemistry and structure actitivity relationship, followed by the evaluation of adrenergic activators and inhibitors, and discussing their mode of action. The most voluminous part is the chapter dealing with the systemic pharma­ cology of these agents analyzing the effects on the central nervous system, on the autonomic nervous system, on the cardiovascular, the respiratory, the digestive, the endocrine system, on the skeletal muscle, and on metabolism. Kinetics and bio­ transformation, further toxic effects are discussed in the following chapters. A special chapter on clinical features concludes the monograph.

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Section I: General Considerations.- 1 Chemistry of Alpha- and Beta-Adrenoceptor Agonists and Antagonists.- A. Introduction.- B. Beta-Adrenergic Agonists.- I. Subclassification of Beta-Adrenoceptors.- II. Structure-Activity Relationships.- 1. Substitution on the Amine Group.- 2. Substitution on the Aromatic Ring.- 3. Side Chain Substitution; Conformation of Phenylethanolamines.- 4. Phenoxypropanolamines.- C. Beta-Adrenergic Antagonists.- I. Potency and Tissue Selectivity.- 1. Side Chain Variations.- 2. Substitution on the Amino Group.- 3. Substitution on the Aromatic Ring.- II. Intrinsic Sympathomimetic Activity.- III. Membrane-Stabilizing Activity.- D. Alpha-Adrenergic Agonists.- E. Subclassification of Alpha-Adrenoceptors.- F. Alpha-Adrenergic Antagonists.- I. Ergot Derivatives.- II. Haloalkylamines; Irreversible Alpha-Blockade.- III. Phenoxyalkylamines and Benzodioxans.- IV. Dibenzazepines and Dibenzazocines.- V. Imidazolines and Related Heterocycles.- VI. Phenylethanolamines.- VII. Piperazines, Piperidines, and Related Heterocycles.- VIII. Yohimbine.- IX. Neuroleptic Drugs.- References.- 2 Sympathomimetic Amine-Induced Responses of Effector Organs Subserved by Alpha-, Beta1-, and Beta2-Adrenoceptors.- A. Introduction.- B. Alpha-Adrenoceptor-Mediated Responses.- I. Vasoconstriction.- II. Spleen Smooth Muscle.- III. Uterus.- IV. Seminal Vesicles.- V. Retractor Penis.- VI. Eye.- VII. Nictitating Membrane.- VIII. Liver.- 1. Glycogenolysis.- 2. Gluconeogenesis.- IX. Intestinal Smooth Muscle.- X. Additional Delineations.- C. Beta1-Adrenoceptor-Mediated Responses.- I. Cardiac Excitation.- II. Cardiac Glycogenolysis.- III. Vascular Smooth Muscle.- 1. Coronaries.- 2. Intestinal Smooth Muscle.- IV. Kidney Renin Release.- V. Adipose Tissue.- 1. White Adipose Tissue Lipolysis.- 2. White Adipose Tissue Lipogenesis.- 3. Brown Adipose Tissue Calorigenesis (Nonshivering Thermogenesis).- VI. Salivary Gland Secretion.- VII. Additional Observations.- D. Beta2-Adrenoceptor-Mediated Responses.- I. Vascular Smooth Muscle Relaxation.- II. Tracheal and Bronchial Smooth Muscle.- 1. Relaxation.- 2. Antianaphylaxis.- III. Skeletal Muscle.- 1. Contraction.- 2. Glycogenolysis (Lacticacidemia).- IV. Potassium Uptake (Hypokalemia).- V. Urinary Bladder.- VI. Uterus.- VII. Insulin Release.- VIII. Gall Bladder.- IX. Vas Deferens.- X. Rat Diaphragm.- XI. Additional Observations.- E. Summary.- References.- 3 Evaluation of Adrenergic Alpha- and Beta-Receptor Activators and Adrenergic Alpha- and Beta-Receptor Blocking Agents.- A. In Vivo Tests.- B. Organ-Perfusion Tests.- C. Isolated Tissues for Evaluation of Adrenergic Drugs.- D. Quantitation of Agonists and Factors Which Affect the Quantitation.- E. Design of an Experiment.- F. Base Line Problems.- G. Analysis of Data.- H. Factors Which Influence the Shapes and Slopes of the Dose-Response Curves of Sympathomimetic Substances.- I. Stereoisomeric Forms.- II. Indirect Action.- III. Density of Adrenergic Innervation.- IV. Distribution of Adrenoceptors.- V. Dose-Response Curves and Ca2+Ions.- VI. Enzymatic Degradation and Drug Disposition.- VII. Miscellaneous Factors.- I. Procedures for Determination of Dissociation Constants (KA) of Agonists.- J. Evaluation of Adrenergic Blockers and Associated Experimental Complications.- K. Evaluation of Adrenergic Drugs in Subcellular Fractions.- L. Concluding Remarks.- References.- 4 Evaluation of Agents That Release or Modify Release of Adrenergic Transmitter.- A. General Considerations.- I. Adrenergic Transmitter-Releasing Agents.- 1. Ganglion Stimulants.- II. Drugs Causing Impaired Transmitter Release.- 1. Major Classes.- 2. The Evaluation of Adrenergic Neurone-Blocking Agents.- 3. The Evaluation of Agents that Deplete Noradrenaline.- 4. Inhibition of Noradrenaline Synthesis.- 5. Evaluation of False Transmitter Substances.- 6. Evaluation of Presynaptic Alpha-Adrenoceptor Agonists.- 7. Other Presynaptic Systems that Reduce Transmitter Release.- B. Some Prefered Methods and Their Use in Evaluating Drugs.- I. Cat Spleen: Release of Adrenergic Transmitter and Motor Responses.- 1. Method.- 2. Evaluation of Drugs.- II. Rabbit Pulmonary Artery: Release of Adrenergic Transmitter and Contractile Response.- 1. Method.- 2. Evaluation of Drugs.- III. Vas Deferens Preparations: Contractions and the Release of Adrenergic Transmitter.- 1. Method.- 2. Evaluation of Drugs.- IV. Perfused Mesenteric Artery of the Rat: Vasoconstrictor Response.- 1. Method.- 2. Evaluation of Drugs.- V. Pithed Rat: Cardiovascular Responses to Sympathetic Activation.- 1. Method.- 2. Evaluation of Drugs.- VI. Anaesthetised Cat: Cardiovascular and Nictitating-Membrane Responses and Reference to Isolated Nictitating-Membrane Preparations.- 1. Methods.- 2. Evaluation of Drugs.- VII. Nictitating-Membrane Relaxation in Unanaesthetised Cats.- VIII. Ptosis in Mice.- IX. Cardiovascular Studies.- 1. Method.- 2. Evaluation of Drugs.- References.- 5 Catecholamine Receptors on Nerve Terminals.- A. Introduction.- B. Prejunctional Alpha-Adrenoceptors on Noradrenergic Nerve Terminals.- I. General Considerations.- II. Effects of Antagonists on Prejunctional Alpha-Adrenoceptors.- 1. Alpha-Adrenoceptor Antagonists and Hypertension.- III. Effects of Agonists on Prejunctional Alpha-Adrenoceptors.- IV. Effects of Partial Agonists on Prejunctional Alpha-Adrenoceptors.- V. Characterization of Prejunctional Alpha-Adrenoceptors.- 1. Localization of Prejunctional Alpha-Adrenoceptors.- 2. Mechanisms of Coupling of Prejunctional Alpha-Adrenoceptors to Inhibition of Transmitter Release.- 3. Differences Between Prejunctional and Postjunctional Alpha-Adrenoceptors.- VI. Inhibitory Feedback Effects of Transmitter on Prejunctional Alpha-Adrenoceptors.- 1. Normal Noradrenergic Transmission.- 2. Effect of Blockade of Transmitter Reuptake.- 3. Effects of Depletion of Noradrenaline Transmitter Stores.- 4. Effect of False Transmitters.- C. Prejunctional Beta-Adrenoceptors on Noradrenergic Nerve Terminals.- I. Effects of Beta-Adrenoceptor Agonists on Noradrenergic Transmission.- II. Effects of Beta-Adrenoceptor Antagonists on Noradrenergic Transmission.- III. A Facilitatory Feedback Loop Through Prejunctional Beta-Adrenoceptors in Noradrenergic Transmission.- 1. Normal Transmission.- 2. Possible Role of Prejunctional Beta-Adrenoceptors in Hypertension.- D. Prejunctional Dopamine Receptors on Noradrenergic Nerve Endings.- I. Possible Relevance of Prejunctional Dopamine Receptors in Understanding Clinical Phenomena.- E. Catecholamine Rec…