Ergot alkaloids and related compounds

摘要: I Introduction to the Pharmacology of Ergot Alkaloids and Related Compounds as a Basis Their Therapeutic Application.- II Chemical Background.- A. Occurrence, Biosynthesis, Production.- 1. Presence in Plant Kingdom.- 2. Biogenesis.- 3. B. Structure Synthesis Natural Alkaloids.- General Structural Aspects.- C. Modifications Lysergic Acid Half Substitutions Position 1.- 2.- Transformations Positions 4 5.- 4. Replacement N-Methyl Group 6 by Other Substituents.- 5. Reactions Involving 7.- 6. Carboxylic Function d-Lysergic Acid.- 7. at 8.- 8. Derivatives 6-Methyl-8-ergolene-8-carboxylic 9. on Double Bond 9, 10.- 10. Substitution Benzene Ring.- D. Modification Peptide Part The Aci-Rearrangement.- Analoga l-Proline Amino Acids Synthetic Modified 5?.- E. Some Analytical Tools for Determination Separation Assay F. Subject Index.- G. References.- III Basic Pharmacological Properties.- Introduction.- Competitive Drug Antagonism.- Corollaries Affinity Intrinsic Activity (Efficacy).- Receptor Classification.- Noncompetitive Actions 5-HT Receptors.- Extraneuronal Effects Metabolism.- Neuronal 5-HT-Sensitive Enzyme Systems.- Dopamine Interaction With Indirect Effects.- Dopamine-Sensitive Receptors Mediating Hormone Secretion.- Adrenoceptors.- Mediated Peripheral ?-Adrenoceptors.- Depletion Noradrenaline From Tissues Release Theories Mechanism "Overflow".- Responses Organs Stimulation Sympathetic Innervation.- Shape Ergotamine Dihydroergotamine Relation Acetylcholine Histamine H. Prostaglandins.- Interference Endogenous Prostaglandin Synthesis.- J. Smooth Muscle Miscellaneous Mechanisms.- Enhancement Biogenic Amines Vascular Muscles.- Agents Nonvascular K. Biochemical Identification Specific Binding Sites Central Nervous System.- Compounds.- L. IV Uterus.- Uterine Motor Activity.- Dihydrogenated Acid-Amides.- V Heart Circulation.- Systemic Blood Pressure.- Nature Effect.- Pressure Control Carotid Sinus Impulse Transmission Sino-Aortic Nerves.- Catecholamines 5-Hydroxytryptamine.- Mechanisms Involved Hypotensive Action.- Pressor Hemodynamic Regional Hemodynamics.- Limb Vessels.- Cranial Renal Mesenteric Coronary Heart.- Mammals.- Amphibia.- Molluscs.- Pharmacologic Clinical Use Orthostatic Hypotension.- Venous Thrombosis.- Shock.- Migraine.- VI Early Evidence Convulsive Ergotism Man.- Description Animals.- Question "Toxic" versus "Therapeutic" Dose.- Whole-Animal Studies.- Behavioral Excitation.- Depression.- Centrally Depressant Drugs.- Anticonvulsant Electroencephalogram.- Cerebral Flow.- Body Temperature.- Emesis.- Synaptic Transmission: Catecholaminergic Criteria Antagonism Level.- Agroclavine-Type Derivatives.- Ergometrine.- D-LSD, 2-Br-LSD, Methysergide.- PRT 17-402.- Ergocornine.- Bromocriptine.- Ergopeptine Efficacy Antiparkinsonian Agents.- Serotoninergic D-LSD.- 2-Br-LSD.- Brain Cyclic Adenosine Monophosphate.- Triphosphate Metabolism Brain.- Transformation Biosubstrates Demethylation, Acetylation Glucuronoconjugation.- VII Senile Insufficiency.- Terminology, Etiology, Pathology Aging Process Terminology.- Definition.- Etiology Pathology.- Research Techniques Used Studies Methods Measuring Bloodflow Assessment Function.- Electroencephalography.- Results Metabolic Summary.- VIII Hallucinogenic Discovery LSD.- LSD Somatic Actions.- Psychic Human EEG.- Laboratory Investigations.- Tolerance Inhibitors Reaction.- Side-Effects Complications.- Illicit Addiction.- Applications Adjuvant Psychotherapy.- Psychedelic Therapy.- Psychoses.- Children.- Terminal Cancer Patients.- Analogues Tested Isomers.- Hydrogenated Unsubstituted Monosubstituted Amide Disubstituted Ring-Substituted Ololiuqui.- Discussion.- Cross-Tolerance.- IX Influence Endocrine Animal Data.- Pituitary Hormones.- X In Vitro Liver.- Adipose Tissue.- Various Tissues.- Intact Animals Men.- Catecholamine-Stimulated Carbohydrate Mobilization.- Lipolysis.- Processes.- Stress-Stimulated Parameters.- Adrenalectomy or Sympathectomy.- Glucose Galactose Tolerance.- Serotonin Pancreas, Hypophysis, Thyroidea.- Alone XI Biopharmaceutical Aspects. Methods, Pharmacokinetics, Bioavailability.- Radiotracer Methods.- Nonradioisotopic Physicochemical Radioimmunoassay.- Pharmacokinetics.- Experiments Interactions Properties Which May Affect Enteral Absorption.- Synopsis.- Experiments.- Biotransformation Molecule.- Cytochrome P 450.- Conclusions Prospects.- XII Toxicologic Considerations.- Toxicity.- Reproductive Implantation Pregnancy.- Embryonic Fetal Development.- Lactation Offspring.- Potential Genetic Conclusions.- Leading Enhanced Disease Concomitant Medication.- Authors Index.