1 Monoamine Oxidase Inhibitors: Animal Pharmacology.- 1. Introduction.- 1.1. Localization.- 1.2. Function.- 1.3. Mechanisms.- 2. Inhibition of 5-HT and Catecholamine Synthesis.- 3. Inhibition of Spontaneous Firing of 5-HT Neurons.- 4. Inhibitory Effects on Paradoxical Sleep and Pontogeniculooccipital Waves.- 5. Effects on Growth and Development.- 6. Inhibition of Ovulation.- 7. Effects on Lordosis.- 8. Effects on Male Copulatory Behavior.- 9. 5-HT-Dependent Behavioral Syndromes.- 9.1. MAOI plus Reserpine or Tetrabenazine.- 9.2. MAOI plus L-Tryptophan.- 9.3. MAOI plus 5-HTP.- 9.4. MAOI plus 5-HT-Uptake Inhibitor.- 10. Potentiation of Indoleamine Hallucinogens.- 11. Tryptamine Potentiation.- 12. Potentiation of Phenethylamine Hallucinogens.- 13. Hypotensive Effects.- 13.1. The False-Transmitter Hypothesis.- 13.2. Centrally Mediated Reduction of Blood Pressure.- 14. Tyramine Potentiation.- 15. Interactions of the MAOIs with Reserpine and Tetrabenazine.- 16. Anticonvulsant Actions of MAOIs.- 16.1. Electroshock and Metrazol Convulsions.- 16.2. Audiogenic Seizures.- 16.3. Other Types of Seizures.- 16.4. Conclusions.- 17. References.- 2 Monoamine Oxidase, Monoamine-Oxidase-Inhibiting Drugs, and Human Behavior.- 1. Introduction.- 2. MAO-Inhibiting Drugs: Biologic, Physiologic, and Behavioral Effects in Man.- 2.1. Monoamine Changes during MAO-Inhibitor Administration to Man.- 2.2. Physiological Changes during MAO-Inhibitor Treatment.- 2.3. Behavioral Changes during MAO-Inhibitor Administration to Man.- 3. Monoamine Oxidase in Human Brain and Other Tissues.- 4. Human Platelet Monoamine Oxidase.- 4.1. Characteristics of Human Platelet Monoamine Oxidase.- 4.2. Genetic Basis for Individual Differences in Platelet MAO Activity.- 4.3. Factors Influencing Platelet MAO Activity.- 4.4. Drug Effects on Platelet MAO Activity.- 4.5. Associations between Platelet MAO Activity and Various Human Disorders.- 5. Possible Association between Platelet MAO Activity and General Personality and Behavioral Factors.- 6. References.- 3 Tricyclic and Monoamine Oxidase Inhibitor Antidepressants: Structure-Activity Relationships.- 1. Introduction.- 1.1. Background.- 1.2. Purposes of this Review and a Limitation.- 2. Tricyclic and Related Compounds.- 2.1. Neuronal Membrane Mechanisms for the Uptake of Biogenic Amines.- 2.2. Inhibition of Norepinephrine Uptake.- 2.3. Inhibition of Catecholamine Uptake into Dopaminergic Neurons.- 2.4. Inhibition of Serotonin Uptake.- 2.5. Relationship between Inhibition of the Uptake of Biogenic Amines and Antidepressant Activity In Vivo : Influence of Structural Modifications.- 3. Monoamine Oxidase Inhibitors.- 3.1. The Active Site of Monoamine Oxidase.- 3.2. Structure-Activity Relationships among Substrates of Monoamine Oxidase.- 3.3. Multiple Substrate-Binding Sites.- 3.4. General Structural Requirements for Monoamine Oxidase Inhibition.- 3.5. Structure-Activity Relationships among Inhibitors of Monoamine Oxidase.- 4. MAOIs as Inhibitors of the Uptake of Biogenic Amines and Tricyclic Compounds as Inhibitors of Monoamine Oxidase.- 4.1. MAOIs as Inhibitors of Amine Uptake.- 4.2. Tricyclic Compounds as MAOIs.- 5. Summary and Perspective.- 6. References.- 4 Tricyclic Antidepressants: Animal Pharmacology (Biochemical and Metabolic Aspects).- 1. Introduction.- 2. Pharmacologic Test Procedures Predicting Clinical Antidepressant Activity.- 2.1. Potentiation of Exogenous and Endogenous Catecholamines at Peripheral Adrenergic Receptor Sites.- 2.2. Potentiation of Various Central Effects Elicited by Amphetamine-like Drugs.- 2.3. Antagonism of Guanethidine-Induced Catecholamine Depletion and Adrenergic Neuron Blockade.- 2.4. Antagonism of the Reserpine-like Syndrome in Rodents.- 2.5. Blockade by Tricyclic Antidepressants of the Uptake of Catecholamines and/or 5-HT.- 3. Mode of Interaction of Tricyclic Antidepressants with Adrenergic Mechanisms.- 4. Interaction of Tricyclic Antidepressants with Other Drugs.- 5. Effect of Tricyclic Antidepressants on Adaptive Regulation at Pre- and Postsynaptic Sites.- 6. Metabolic Fate of Tricyclic Antidepressants.- 7. Some General Considerations on iV-Demethylation of Tricyclic Antidepressants.- 8. Miscellaneous Pharmacologic Effects of Tricyclic Antidepressants.- 9. References.- 5 Tricyclic and Monoamine-Oxidase-Inhibitor Antidepressants: Clinical Use.- 1. Introduction.- 2. Tricyclic Antidepressants: Clinical Studies.- 3. Adverse Effects of Tricyclic Antidepressants.- 4. MAOI: Clinical Studies.- 5. Adverse Effects of the MAOIs.- 6. Treatment of the Acute Episode.- 7. Prophylaxis.- 8. Interactive Effects of Tricyclic Agents and Sociotherapy.- 9. Combined Drug Treatments.- 10. Other Uses of the Antidepressants.- 10.1. Neurotic Disorders.- 10.2. Antidepressants in the So-Called Psychosomatic Disorders.- 10.3. Narcolepsy.- 10.4. Disorders of Childhood.- 10.5. Phobia.- 10.6. Hyperactivity.- 10.7. Enuresis.- 11. Current Practices and Future Needs.- 12. References.- 6 Lithium Pharmacology and Physiology.- 1. Introduction.- 2. Historical Review.- 2.1. Discovery in Basic Chemistry.- 2.2. History of Clinical Uses.- 2.3. Present Uses.- 3. Basic Chemistry and Biophysics.- 3.1. Basic Properties.- 3.2. Lithium and Cell Membranes.- 3.3. Lithium and. Facilitated Diffusion.- 3.4. Lithium and Active Transport.- 4. Mechanism of Action.- 4.1. Intracellular Concentration.- 4.2. Lithium Adenylate Cyclase and Cyclic Adenosine 3?,5?-Phosphate (cAMP).- 4.3. Cellular Magnesium and Calcium.- 4.4. Synaptic Release and Synthesis of Catecholamines.- 4.5. Indoleamines and Lithium.- 4.6. Effect of Lithium on Acetylcholine.- 4.7. Lithium and GABA.- 4.8. Lithium and the Electrolyte/Membrane Theory of Affective Disorders.- 4.9. Integration of the Mechanisms of Action of Lithium and the Theories of Affective Disorders.- 5. Physiology.- 5.1. Absorption.- 5.2. Distribution.- 5.3. Excretion.- 5.4. Interactions with Other Cations.- 6. Interactions with Pharmaceuticals.- 6.1. Concurrent Use of Diuretics.- 6.2. Lithium and Haloperidol.- 6.3. Lithium and Insulin.- 6.4. Lithium and Tricyclic Antidepressants.- 6.5. Lithium and the MAOI-Tranylcypromine.- 6.6. Lithium and Diphenylhydantoin.- 7. Effects on Clinical Tests.- 7.1. ECG(EKG).- 7.2. EEG.- 7.3. WBC.- 7.4. Serum Sodium and Potassium.- 7.5. Serum Magnesium and Calcium.- 8. Conclusion.- 9. References.- 7 Lithium: Clinical Considerations.- 1. Introduction.- 1.1. Indications.- 2. Lithium in Mania.- 2.1. Uncontrolled and Single-Blind Studies.- 2.2. Controlled Studies.- 3. Lithium in Acute Endogenous Depression.- 4. Use of Lithium in Psychiatric Disorders Other Than Mania or Depression.- 4.1. Lithium In Tardive Dyskinesia.- 5. Use of Lithium in Disorders of Childhood and Adolescence.- 5.1. Hyperactive Children.- 5.2. Mood Disorders.- 6. Preparations, Dosage, and Control.- 6.1. Preparations.- 6.2. Stabilization of a Manic Episode.- 6.3. Maintenance Treatment.- 7. Toxicology of the Lithium Ion.- 7.1. Mild-Moderate Toxic Side Effects: Minor Lithium Intolerance.- 7.2. Lithium Poisoning.- 7.3. Treatment of Lithium Poisoning.- 7.4. General Considerations.- 7.5. Complications of Lithium Treatment.- 7.6. Neurological Side Effects of Lithium Maintenance.- 7.7. “Irreversible” Lithium Toxicity.- 8. References.- 8 Lithium Prophylaxis and Experimental Rubidium Therapy in Affective Disorders.- 1. Factors in Assessing Prophylaxis.- 2. Methodology of Prophylactic Trials.- 3. Early Trials.- 4. Double-Blind Trials.- 5. Prophylaxis in Depression.- 6. Considerations in Prophylaxis: Summary.- 7. The life Table.- 8. Rubidium in Psychiatry.- 9. Recent Studies.- 10. Endogenous Rubidium.- 11. Chronic Administration.- 12. Rubidium-Lithium Interactions.- 13. A Membrane Transport Hypothesis.- 14. References.