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• W2025370022 abstract "1 The inotropic effects of (−)−4-(3-t-butylamino-2-hydroxypropoxy)benzimidazol-2-one ((−)−CGP 12177), an antagonist for β1- and β2-adrenoceptors as well as an agonist for β3-adrenoceptors, were investigated on paced preparations of isolated right atrial appendages obtained from patients without advanced heart failure undergoing open heart surgery. 2 In the presence of (−)−propranolol (200 nM), (−)−CGP 12177 increased contractile force with a -log EC50, M, of 7.3. The maximum effects of (−)−CGP 12177 amounted to 15% and 11% of the effects of (−)−isoprenaline (400 μm) and of CaCl2 (6.75 mM) respectively. 3 (—)-Bupranolol 1 μm, an antagonist with a pKB of ∼7.5 for β3-adrenoceptors, antagonized surmountably the positive inotropic effects of (—)-CGP 12177 (in the presence of 200 nM (−)−propranolol) with an apparent pKB of 7.3. 4 The potent positive inotropic effects of (−)−CGP 12177 and their resistance to blockade by (−)−propranolol but antagonism by (−)−bupranolol are consistent with the existence in human atrial myocardium of a minor third β-adrenoceptor population, possibly related to β3-adrenoceptors." @default.
• W2025370022 created "2016-06-24" @default.
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• W2025370022 date "1996-01-01" @default.
• W2025370022 modified "2023-10-14" @default.
• W2025370022 title "(—)‐CGP 12177‐induced increase of human atrial contraction through a putative third β‐adrenoceptor" @default.
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• W2025370022 doi "https://doi.org/10.1111/j.1476-5381.1996.tb15159.x" @default.
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