The selectivity of beta-adrenoceptor antagonists on isoprenaline-induced changes in heart rate, blood pressure, soleus muscle contractility and airways function in anaesthetized cats

British Journal of Pharmacology
L G LettsL R Williams

Abstract

The beta-adrenoceptor antagonist of propranolol, metoprolol, atenolol and butoxamine in anaesthetized cats has been measured and compared with the activity of four synthetic phenylethanolamine derivatives. The effects of isoprenaline on four parameters in the anaesthetized cat: heart rate, blood pressure, soleus muscle contractility and airway reactance, were measured and the modification of the isoprenaline dose-response relation by each of the antagonist drugs assessed. Parallel shifts in log dose-response curves for isoprenaline were caused by propranolol for all parameters, by metoprolol and atenolol for each parameter except blood pressure, and butoxamine for each except soleus muscle and heart rate. Selectivity of action of the antagonists between different organs was measured by comparing DR10 values, computed from isoprenaline dose-ratios. Propranolol was the most potent antagonist and showed slight selectivity of action on soleus muscle compared with heart. Atenolol and metoprolol were approximately equipotent and were cardioselective at low doses only. Butoxamine was the least potent antagonist and possessed non-beta-adrenoceptor effects on the parameters measured. Each of the new compounds, 4'-bromo-2'-methoxy-N-isop...Continue Reading

References

Oct 1, 1978·Journal of Medicinal Chemistry·L R WilliamsG L Letts
Nov 1, 1978·Clinical and Experimental Pharmacology & Physiology·J D Fitzgerald, S R O'Donnell
Jun 1, 1971·European Journal of Pharmacology·J R BoissierP Viars
Feb 1, 1973·Life Sciences. Pt. 1: Physiology and Pharmacology·B AbladL Ek
Jan 1, 1968·British Journal of Pharmacology and Chemotherapy·D Dunlop, R G Shanks
Sep 15, 1969·Experientia·J BergmanK Wetterlin
Mar 1, 1959·British Journal of Pharmacology and Chemotherapy·O ARUNLAKSHANA, H O SCHILD

Citations

Apr 16, 1986·European Journal of Pharmacology·H J SchliepG Haeusler
Feb 23, 2012·American Journal of Physiology. Endocrinology and Metabolism·Rebecca Berdeaux, Randi Stewart

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Adrenergic beta-Antagonists
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