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InhaltsangabeAbstracts.- 1 Introduction: Calcium Entry Blockers (CEBs).- 1.1 History of Calcium Entry Blocker New Drug Discovery.- 1.1.1 Calcium Entry Channels.- 1.1.2 Calcium Channel Determinates of Drug Action.- 1.1.3 Alpha-2 Receptor Activated Channels.- 1.1.4 Labeling Calcium Entry Channels.- 1.2 Nomenclature and Classification.- 1.3 Definitional Characteristics.- 1.4 Screening Philosophy.- 1.5 Methodological Notes for Screening Vascular Effects.- 2 Current Calcium Entry Blocker.- 2.1 Status of CEB New Drug Discovery.- 2.1.1 First Generation "Standard Triad" Compounds.- 2.1.2 Other Vintage Compounds.- 2.1.3 Second Generation CEBs.- 2.1.4 New or Little Studied CEBs.- 2.1.5 Compounds with Secondary Calcium Entry Blocking Actions.- 2.1.6 Intracellular Calcium Antagonists.- 2.1.7 Status: "Conclusion".- 2.2 Additional Sites of Action.- 2.2.1 Inhibition of Phosphodiesterase.- 2.2.2 Interaction with Calmodulin.- 2.2.3 Inhibition of Intracellularly Released Calcium.- 2.2.4 Stimulation of Calcium Extrusion.- 2.2.5 Interaction with Alpha Adrenoceptors.- 3 Preclinical Pharmacology.- 3.1 Vasodilator Effects of CEBs.- 3.2 Antihypertensive Effects of CEBs.- 3.3 CEB Effects on Myocardial Rate and Rhythm.- 3.4 Anti-Ischemic/Myocardial Protective Effects of CEBs.- 3.5 Cytoprotective Effects of CEBs in Hepatic Injury.- 3.6 Cytoprotective Actions of CEBs in Models of Cerebral Ischemic Injury.- 3.7 Effects of CEBs on Airway Smooth Muscle and Mast Cell Mediator Release.- 3.8 CEBs in Atherosclerosis.- 3.9 Effects of CEBs on Platelet Aggregation.- 3.10 Effects of CEBs on Red Blood CElls.- 3.11 CEBs and Neutrophil Function.- 3.12 Endocrine Effects of CEBs.- 4 Therapeutic Indications.- 4.1 Angina Pectoris.- 4.1.1 Chronic Stable Angina.- 4.1.2 Vasospastic Angina.- 4.1.3 Unstable Angina.- 4.1.4 Acute Myocardial Infarction.- 4.2 Arterial Hypertension.- 4.2.1 Essential Hypertension.- 4.2.2 Pulmonary Hypertension.- 4.3 Vascular Disease.- 4.3.1 Peripheral Vascular Disease.- 4.3.2 Cerebral Vascular Disease.- 4.4 Congestive Heart Failure.- 4.5 Myocardial Arrhythmias.- 4.5.1 Artial Arryhthmias.- 4.5.2 Ventricular Arrhythmias.- 4.6 Asthma.- 4.7 Other Therapeutic Indications.- 4.7.1 Cardiovascular Indications.- 4.7.2 Non-Cardiovascular Indications.- 4.7.3 Miscellaneous "NEW" Possibilities.- 5 Adverse Effects.- 6 Perspectives: CEB New Drug Discovery.- 7 Acknowledgement.- 8 References.- Author Index Volumes 1-6.
InhaltsangabeAbstracts.- 1 Introduction: Calcium Entry Blockers (CEBs).- 1.1 History of Calcium Entry Blocker New Drug Discovery.- 1.1.1 Calcium Entry Channels.- 1.1.2 Calcium Channel Determinates of Drug Action.- 1.1.3 Alpha-2 Receptor Activated Channels.- 1.1.4 Labeling Calcium Entry Channels.- 1.2 Nomenclature and Classification.- 1.3 Definitional Characteristics.- 1.4 Screening Philosophy.- 1.5 Methodological Notes for Screening Vascular Effects.- 2 Current Calcium Entry Blocker.- 2.1 Status of CEB New Drug Discovery.- 2.1.1 First Generation "Standard Triad" Compounds.- 2.1.2 Other Vintage Compounds.- 2.1.3 Second Generation CEBs.- 2.1.4 New or Little Studied CEBs.- 2.1.5 Compounds with Secondary Calcium Entry Blocking Actions.- 2.1.6 Intracellular Calcium Antagonists.- 2.1.7 Status: "Conclusion".- 2.2 Additional Sites of Action.- 2.2.1 Inhibition of Phosphodiesterase.- 2.2.2 Interaction with Calmodulin.- 2.2.3 Inhibition of Intracellularly Released Calcium.- 2.2.4 Stimulation of Calcium Extrusion.- 2.2.5 Interaction with Alpha Adrenoceptors.- 3 Preclinical Pharmacology.- 3.1 Vasodilator Effects of CEBs.- 3.2 Antihypertensive Effects of CEBs.- 3.3 CEB Effects on Myocardial Rate and Rhythm.- 3.4 Anti-Ischemic/Myocardial Protective Effects of CEBs.- 3.5 Cytoprotective Effects of CEBs in Hepatic Injury.- 3.6 Cytoprotective Actions of CEBs in Models of Cerebral Ischemic Injury.- 3.7 Effects of CEBs on Airway Smooth Muscle and Mast Cell Mediator Release.- 3.8 CEBs in Atherosclerosis.- 3.9 Effects of CEBs on Platelet Aggregation.- 3.10 Effects of CEBs on Red Blood CElls.- 3.11 CEBs and Neutrophil Function.- 3.12 Endocrine Effects of CEBs.- 4 Therapeutic Indications.- 4.1 Angina Pectoris.- 4.1.1 Chronic Stable Angina.- 4.1.2 Vasospastic Angina.- 4.1.3 Unstable Angina.- 4.1.4 Acute Myocardial Infarction.- 4.2 Arterial Hypertension.- 4.2.1 Essential Hypertension.- 4.2.2 Pulmonary Hypertension.- 4.3 Vascular Disease.- 4.3.1 Peripheral Vascular Disease.- 4.3.2 Cerebral Vascular Disease.- 4.4 Congestive Heart Failure.- 4.5 Myocardial Arrhythmias.- 4.5.1 Artial Arryhthmias.- 4.5.2 Ventricular Arrhythmias.- 4.6 Asthma.- 4.7 Other Therapeutic Indications.- 4.7.1 Cardiovascular Indications.- 4.7.2 Non-Cardiovascular Indications.- 4.7.3 Miscellaneous "NEW" Possibilities.- 5 Adverse Effects.- 6 Perspectives: CEB New Drug Discovery.- 7 Acknowledgement.- 8 References.- Author Index Volumes 1-6.
