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Produktbild: The alpha-1 Adrenergic Receptors

The alpha-1 Adrenergic Receptors

Aus der Reihe The Receptors

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Beschreibung

Details

Einband

Taschenbuch

Erscheinungsdatum

05.10.2011

Verlag

Humana Press

Seitenzahl

544

Maße (L/B/H)

22,9/15,2/3,1 cm

Gewicht

812 g

Auflage

1987

Sprache

Englisch

ISBN

978-1-4612-8936-4

Beschreibung

Details

Einband

Taschenbuch

Erscheinungsdatum

05.10.2011

Verlag

Humana Press

Seitenzahl

544

Maße (L/B/H)

22,9/15,2/3,1 cm

Gewicht

812 g

Auflage

1987

Sprache

Englisch

ISBN

978-1-4612-8936-4

Herstelleradresse

Springer-Verlag GmbH
Tiergartenstr. 17
69121 Heidelberg
DE

Email: ProductSafety@springernature.com

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  • Produktbild: The alpha-1 Adrenergic Receptors
  • Section 1: Historical Perspectives.- 1 alpha-1 Adrenergic Receptors: A Historical Perspective.- 1. Introduction.- 2. Adrenotropic Receptors.- 3. Receptor Blockers.- 4. Recent Developments.- 5. Conclusion.- References.- Section 2: Characterization of the Receptor and Its Binding Site.- 2 Biochemistry and Pharmacology of the alpha-1 Adrenergic Receptor.- 1. Introduction.- 1.1. Overview.- 1.2. Radioligand Binding Studies.- 2. Radioligand Binding Studies in Particulate Fractions.- 2.1. Radioligands.- 2.2. Assay Methods.- 2.3. Comparison of Radioligands.- 2.4. Tissue and Regional Distribution.- 2.5. Effects of Cations, Guanine Nucleotides, and Sulfhydryl Reagents on alpha-1 Adrenergic Receptor Binding.- 2.6. Thermodynamics.- 3. Binding in Intact Cells.- 4. Photoaffinity Labels.- 5. Solubilization and Purification of the alpha-1 Adrenergic Receptor Binding Protein.- 6. Structure of the alpha-1 Adrenergic Receptor.- 7. Concluding Remarks.- References.- 3 Localizing the alpha-1 Adrenergic Receptor in the Central Nervous System: Relating Pharmacology to Structure and Function.- 1. Introduction.- 2. Procedures.- 2.1. Receptor Autoradiography: Application of Ligand Binding Techniques to the Study of Functional Neurochemical Anatomy.- 2.2. Ligands Used to Label the alpha-1 Adrenergic Binding Site: Advantages and Problems.- 3. Localization of alpha-1 Binding Sites in the RatCNS.- 3.1. Autoradiographic Distribution.- 4. Relationship of the Anatomic Distribution of alpha-1 Adrenergic binding Sites to Structure and Function.- 4.1. Relationship of alpha-1 Adrenergic Binding Sites to Central Noradrenergic Pathways.- 4.2. Relationship of the alpha-1 Adrenergic Binding Site Distribution to Functional Neuroanatomy: Hypotheses and Future Directions.- 5. Conclusions.- References.- Section 3: Biochemical Mechanism of Receptor Action.- 4 Ca2+ Utilization in Signal Transformation of alpha-1 Adrenergic Receptors.- 1. Introduction.- 2. Affinity of Ca2+ Channel Blockers for alpha-1 Adrenergic Receptors.- 3. Ca2+ Utilization and alpha-1 Adrenergic Receptor-Mediated Vasoconstriction In Vivo.- 4. Ca2+ Utilization and alpha-1 Adrenergic Receptor-Mediated Vasoconstriction In Vitro.- 4.1. Rabbit Aorta.- 4.2. Rat Aorta.- 4.3. Guinea Pig Aorta.- 4.4. Rabbit Pulmonary Artery.- 4.5. Dog Saphenous Vein.- 4.6. Dog Coronary Artery.- 4.7. Dog Saphenous Artery.- 4.8. Rat Tail Artery.- 4.9. Rabbit Ear Artery.- 4.10. Cerebral Arteries.- 4.11. Portal Veins.- 4.12. Renal Arteries/Renal Arterial Bed.- 4.13. Mesenteric Artery/Mesenteric Arterial Bed.- 4.14. Perfused Rat Hindquarters.- 4.15. Rat Anococcygeus Muscle.- 4.16. Electrophysiology of alpha-1 Adrenergic Receptor-Induced Smooth Muscle Contraction.- 5. Receptor Reserve and Susceptibility of alpha-1 Adrenergic Receptor-Mediated Vasoconstriction to Inhibition by Ca2+ Entry Blockade.- 6. Closing Remarks.- References.- 5 Phosphoinositides and alpha-1 Adrenergic Receptors.- 1. The Phosphoinositide Effect.- 1.1. Introduction.- 1.2. Pathways of the PI Effect.- 1.3. Relationship of Inositol Lipid Turnover to alpha-1 Adrenergic Receptors.- 2. Phosphoinositides and Stimulus-Response Coupling.- 2.1. Relationship of Inositol Lipid Turnover to Calcium Mobilization.- 2.2. Inositol Trisphosphate and Calcium Release.- 2.3. Calcium Entry.- 2.4. Diacylglycerol as a Messenger of the alpha-1 Adrenergic Receptor.- 3. Coupling of Receptors to Phospholipase C.- 4. Summary and Conclusions.- References.- Section 4: Correlation of Receptor Binding and Function.- 6 Structure-Activity Relationships for alpha-1 Adrenergic Receptor Agonists and Antagonists.- 1. Introduction.- 2. Classification of alpha-1 Adrenergic Receptor Agonists.- 3. Affinity and Efficacy of alpha-1 Adrenergic Receptor Agonists.- 4. Stereochemical Requirements of alpha-1 Adrenergic Receptors.- 4.1. Conformational Requirements of alpha-1 Adrenergic Receptors.- 4.2. Configurational Requirements of alpha-1 Adrenergic Receptors.- 5. Structure-Activity Relationships of alpha-1 Adrenergic Receptor Agonists.- 5.1. Phenethylamines.- 5.2. Imidazolines.- 5.3. 2-Aminotetralins: Phenethylamines or Imidazolines.- 6. Structure—Activity Relationships of alpha-1 Adrenergic Receptor Antagonists.- 6.1. Competitive alpha-1 Adrenergic Receptor Antagonists.- 6.2. Irreversible alpha-1 Adrenergic Receptor Antagonists.- 7. Closing Remarks.- References.- 7 Relationship of alpha-1 Adrenergic Receptor Occupancy to Tissue Response.- 1. Introduction.- 2. Existence of Receptor Reserves.- 3. Measurement of Isolated Tissue Responsiveness.- 3.1. Optimal Conditions.- 3.2. Antagonists.- 3.3. Partial Agonists.- 3.4. Full Agonists.- 4. Direct Occupancy Measurements with Radioligands.- 4.1. Tissue Preparation.- 4.2. Experimental Conditions.- 5. Direct Evidence for alpha-1 Adrenergic Receptor Reserve.- 6. Comparison of Binding and Functional Affinity Constants.- 6.1. Affinity Constants for Functional Receptors.- 6.2. Affinity Constants for Radioligand Binding Sites.- 6.3. Comparison of Functional Data with Binding Data.- 6.4. Activation of Phosphatidylinositol Metabolism.- 6.5. Binding and Functional Measurements Performed in the Same Tissues.- 7. Binding Sites and Functional Receptors.- 8. Regulation of Receptor Density and Responsiveness.- 9. Summary.- References.- 8 Heterogeneity of alpha-1 Adrenergic Receptors.- 1. Introduction.- 2. Are There Prejunctional alpha-1 Adrenergic Receptors?.- 3. Are There alpha-Adrenergic Receptors with Characteristics of Both alpha-1 and alpha-2 Subtypes?.- 4. Differential Interaction of Agonists and Antagonists with alpha-1 Adrenergic Receptors.- 5. Differences in Calcium Utilization Among alpha-1 Adrenergic Receptor Agonists.- 6. Conclusions.- References.- 9 Heterogeneity of alpha-Adrenergic Responsiveness in Vascular Smooth Muscle: Role of Receptor Subtypes and Receptor Reserve.- 1. Introduction.- 2. Distribution of alpha-1 and alpha-2 Adrenergic Receptors in the Vascular System.- 2.1. Postjunctional alpha-1 Adrenergic Receptors.- 2.2. Postjunctional alpha-2 Adrenergic Receptors.- 3. Distribution of alpha-Adrenergic Receptors in the Blood Vessel Wall.- 3.1. “Innervation” of alpha-Adrenergic Receptors.- 3.2. Adrenergic Nerves.- 3.3. Endothelial Cells.- 4. Cellular Actions Initiated by alpha-1 Adrenergic Receptors.- 4.1. Membrane Potential.- 4.2. Entry and Release of Intracellular Calcium.- 5. Receptor Reserve and Responses to alpha-1 Adrenergic Receptor Agonists.- 5.1. Theoretical Importance.- 5.2. Receptor Reserve and Calcium Antagonists.- 5.3. Receptor Reserve and Thermoregulation.- 5.4. Receptor Reserve and Acidosis.- 5.5. Receptor Reserve and Vascular Heterogeneity.- 6. Are There Subtypes of alpha-1 Adrenergic Receptors in Vascular Smooth Muscle?.- 6.1. Pulmonary Artery of the Rabbit.- 6.2. Aorta of the Rat.- 6.3. Are There Differences in alpha-1 Adrenergic Receptors Between Species?.- References.- 10 alpha-1 Adrenergic Receptors in the Central Nervous System.- 1. Introduction.- 1.1. Central Noradrenergic Neuronal System.- 1.2. Scope.- 2. Labeling of Central alpha-1 Adrenergic Receptors.- 2.1. Anatomical Distribution.- 2.2. Pharmacological Properties.- 2.3. Plasticity.- 3. Metabolic Consequences of Central alpha-1 Adrenergic Receptor Activation.- 3.1. Synthesis of cyclic AMP.- 3.2. Synthesis of cyclic GMP.- 3.3. Hydrolysis of Phosphoinositides.- 3.4. Modulation of N-Acetyltransferase Activity.- 3.5. Modulation of Effect of Ethanol and ATPase.- 4. Electrophysiological Consequences of Central alpha-1 Adrenergic Receptor Activation.- 4.1. Neurons.- 4.2. Glial Cells.- 4.3. Conclusions.- 5. General Conclusions.- References.- Section 5: Regulation of alpha-1 Adrenergic Receptors.- 11 Regulation of alpha-1 Adrenergic Receptors.- 1. Introduction.- 2. Vascular alpha-1 Adrenergic Receptors.- 2.1. Direct Measurement of Vascular alpha-1 Adrenergic Receptors.- 2.2. Desensitization of Smooth Muscle alpha-1 Adrenergic Receptors.- 2.3. Hypertension.- 3. Hormonal Regulation of Smooth Muscle alpha-1 Adrenergic Receptors.- 4. Regulation of alpna-1 Adrenergic Receptors in Liver.- References.- Section 6: Agents Interacting with alpha-1 Adrenergic Receptors.- 12 Therapeutic Applications of Agents Interacting with alpha-1 Adrenergic Receptors.- 1. alpha-1 Adrenergic Receptor Agonists.- 1.1. Actions on the Heart.- 1.2. Agents Acting on the Vasculature.- 2. alpha-1 Adrenergic Receptor Antagonists.- 2.1. Peripheral alpha-Adrenergic Receptor Blocking Agents as Antihypertensives.- 2.2. Combination of alpha-1 Adrenergic Receptor Blockade with Other Pharmacologic Activities in the Treatment of Hypertension.- 2.3. alpha-1 Adrenergic Receptor in the Management of Pheochromocytoma.- 2.4. alpha-1 Adrenergic Receptor Antagonists in the Treatment of Peripheral Vascular Disease.- 2.5. alpha-1 Adrenergic Receptor Antagonists in the Treatment of Congestive Heart Failure.- 2.6. Adrenergic Receptor Antagonists in the Treatment of Myocardial Ischemic Conditions.- 2.7. alpha-Adrenergic Receptor Antagonists as Antiarrhythmic Agents.- 2.8. alpha-Adrenergic Receptor Antagonists in the Therapy of Circulatory Shock.- 2.9. alpha-1 Adrenergic Receptor Antagonists in the Treatment of Benign Prostatic Hypertrophy.- 3. Conclusion.- References.- Section 7: Future Vistas.- 13 alpha-1 Adrenergic Receptors: Summary and Future Vistas.- 1. Introduction.- 2. Purification and Structure of alpha-1 Adrenergic Receptors.- 3. alpha-1 Adrenergic Receptor Subtypes and Their Localization.- 4. Structure-Activity Relationships.- 5. Receptor Regulation.- 6. Mechanism of alpha-1 Adrenergic Receptor Action.- 7. Conclusion.- References.