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• W2018072556 abstract "1 (−)-Atenolol was used as a tool to assess the function of β1 and β2-adrenoceptors in human heart. Right atrial and left ventricular preparations from patients undergoing open heart surgery were set up to contract isometrically. Membrane particles were prepared for β-adrenoceptor labelling with [3 H]-(−)-bupranolol and adenylate cyclase assays. 2 The positive inotropic effects of (−)-noradrenaline were antagonized to a similar extent by (−)-atenolol in atrial and ventricular preparations. (−)-Atenolol consistently antagonized the effects of (−)-adrenaline to a lesser extent than those of (−)-noradrenaline in atrial preparations. In ventricular preparations (−)-atenolol antagonized the effects of low concentrations of (−)-adrenaline to a lesser extent than those of high concentrations. 3 pKB values (M) of (−)-atenolol, estimated with non-linear analysis from the blockade of the positive inotropic effects of the catecholamines, were 7.4 for β1-adrenoceptors and 6.0 for β2-adrenoceptors. 4 (−)−Atenolol inhibited the binding of [3 H]-(−)-bupranolol to ventricular β1-adrenoceptors with a pKD (M) of 5.9 and to ventricular β2-adrenoceptors with a pKD of 4.6. 5 (−)-Atenolol inhibited the catecholamine-induced adenylate cyclase stimulation in the atrium and ventricle with pKB values of 5.8-6.4 for β1 and pKB values of 4.7-5.7 for β2-adrenoceptors. The binding and cyclase assays suggest a partial affinity loss for (−)-atenolol inherent to membrane preparations. 6 β1 -Adrenoceptors mediate the maximum positive inotropic effects of (−)-noradrenaline in both the atrium and ventricle of man. β2-Adrenoceptors appear to be capable of mediating maximal positive inotropic effects of (−)-adrenaline in atrium. In contrast, ventricular β2-adrenoceptors mediate only submaximal effects of (−)-adrenaline." @default.
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• W2018072556 date "1988-09-01" @default.
• W2018072556 modified "2023-09-27" @default.
• W2018072556 title "Contribution of β1- and β2-adrenoceptors of human atrium and ventricle to the effects of noradrenaline and adrenaline as assessed with (−)-atenolol" @default.
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• W2018072556 doi "https://doi.org/10.1111/j.1476-5381.1988.tb16548.x" @default.
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