188宝金博页面版

Chapter ACardiovascular Activity 1A.1 Cardiovascular Analysis ......... 51A.1.1 In Vitro Methods ................. 51A.1.1.1 α 1 -Adrenoreceptor Binding ....... 51A.1.1.2 α 2 -Adrenoreceptor Binding ....... 54A.1.1.3 Electrically Stimulated Releaseof [ 3 H]Norepinephrinefrom Brain Slices ................. 57A.1.1.4 Imidazoline Receptor Binding ..... 59A.1.1.5 β-AdrenoreceptorBinding ........ 62A.1.1.6 β 1 -AdrenoreceptorBinding ....... 64A.1.1.7 β 2 -AdrenoreceptorBinding ....... 65A.1.1.8 Adenosine A 1 Receptor Binding... 69A.1.1.9 Adenosine A 2 Receptor Binding... 71A.1.1.10 Adenosine A 3 Receptor Binding... 73A.1.1.11 Inhibition of Adenosine Uptakein Human Erythrocytes............ 74A.1.1.12 Inhibition of Vasopeptidases....... 75A.1.1.12.1 Inhibition of the Angiotensin-Converting Enzymein Vitro Purpose and Rationale .... 76A.1.1.12.2 Inhibition of NeutralEndopeptidase (Neprilysin)........ 77A.1.1.13 Quantitative AutoradiographicLocalization of Angiotensin-Converting Enzyme ............... 79A.1.1.14 Angiotensin Antagonism .......... 80A.1.1.14.1 Angiotensin II Receptor Binding .. 80A.1.1.14.2 AT 2 Receptor Binding ............ 84A.1.1.14.3 Angiotensin II Induced Contractionin Isolated Rabbit Aorta ........... 85A.1.1.14.4 Angiotensin II Antagonism in Vivo 86A.1.1.15 Renin-Inhibitory ActivityUsing Human Kidney Reninand a Synthetic Substrate.......... 88A.1.1.16 PAF Binding Assay ............... 90A.1.1.17 Endothelin ....................... 91A.1.1.17.1 General Considerations ........... 911 With contributions to this and the former editions by B.A.Schölkens, H. Gögelein, F.P. Huger, W. Linz, K.A. Rudolphi, K.Wirth.A.1.1.17.2 Evaluation of Endothelin Activity . 92A.1.1.17.3 Endothelin Receptor Antagonismin Vitro........................... 93A.1.1.17.4 Endothelin Receptor Antagonismin Vivo ........................... 95A.1.1.17.5 QuantitativeAutoradiographicLocalizationof Endothelin-1 Receptor.......... 97A.1.1.17.6 Inhibition of EndothelinConverting Enzyme ............... 98A.1.1.18 Nitric Oxide ...................... 101A.1.1.18.1 General Considerationson Nitric Oxide ................... 101A.1.1.18.2 Bioassay of EDRF Release ........ 102A.1.1.18.3 Isolated Arterieswith and Without Endothelium .... 103A.1.1.18.4 Nitric Oxide Formationby Cultured Endothelial Cells ..... 104A.1.1.18.5 Expressionof Nitric Oxide Synthase .......... 107A.1.1.19 Inhibition of Rho Kinase .......... 109A.1.1.20 Inhibition of Na + /H + Exchange.... 109A.1.1.20.1 Inhibition of Na + /H + Exchangein Thrombocytes.................. 111A.1.1.20.2 Inhibition of Na + /H + Exchangein Cholesterol Activated RabbitErythrocytes...................... 111A.1.1.20.3 Sodium Influxinto Cultured Cardiac Myocytes ... 112A.1.1.20.4 Inhibition of Na + /H + Exchangeinto Cultured AorticEndothelial Cells ................. 113A.1.1.20.5 NHE Activity Measured byIntracellular pHin Isolated Ventricular Myocytes... 113A.1.1.20.6 NHE Subtype Specificity.......... 114A.1.1.21 Phosphodiesterases ............... 115A.1.1.21.1 Inhibition of Phosphodiesterase.... 116A.1.1.22 Stimulation of Heart MembraneAdenylate Cyclase ................ 121A.1.1.233 H-Forskolin Binding Assay ...... 123