Synopsis
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 Adrene
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