SELECTIVITY OF β-ADRENOCEPTOR AGONISTS AND ANTAGONISTS ON BRONCHIAL, SKELETAL, VASCULAR AND CARDIAC MUSCLE IN THE ANAESTHETIZED CAT

作者: G.H. APPERLEY , M.J. DALY , G.P. LEVY

DOI: 10.1111/J.1476-5381.1976.TB07473.X

关键词:

摘要: 1 The potencies of fifteen beta-adrenoceptor agonists widely differing chemical structures were compared with that (-)-isoprenaline on bronchial muscle, soleus blood pressure and heart rate in the anaesthetized cat. antagonist propranolol practolol determined against same model. 2 (-)-Isoprenaline was most potent agonist its action essentially unselective. Thus, all four parameters minimal effective dose 0.003-0.01 mug/kg maximal or near responses produced by 0.3-1 mug/kg. Trimetoquinol also an unselective agonist. 3 For thirteen remaining fourteen agonists, potency similar muscle but significantly lower rate. 4 - AH 7616 (4-hydroxy-alpha1-[[(1-methyl-3,3-diphenyl-propyl)amino]-methyl]-m-xylene-alpha1, alpha3-diol, acetate) less than other parameters; addition, it clearly when 5-hydroxytryptamine (5-HT) used to induce bronchospasm. However, acetylcholine instead 5-HT very similar. may therefore possess a specific addition action. 5 test longer acting this particularly true trimetoquinol soterenol. 6 almost identical slightly heart. Practolol 10-12 times more pressure. 7 These findings suggest not be possible separate bronchodilating tremorenhancing properties agonists. results antagonists are accord Lands' dual sub-classification.

参考文章(32)
STELLA R. O'DONNELL, JANET C. WANSTALL, Potency and selectivity in vitro of compounds related to isoprenaline and orciprenaline on β-adrenoceptors in the guinea-pig British Journal of Pharmacology. ,vol. 52, pp. 407- 417 ,(1974) , 10.1111/J.1476-5381.1974.TB08610.X
A. M. LANDS, A. ARNOLD, J. P. MCAULIFF, F. P. LUDUENA, T. G. BROWN, Differentiation of receptor systems activated by sympathomimetic amines. Nature. ,vol. 214, pp. 597- 598 ,(1967) , 10.1038/214597A0
E. J. CORNISH, R. C. MILLER, Comparison of the β-adrenoceptors in the myocardium and coronary vasculature of the kitten heart Journal of Pharmacy and Pharmacology. ,vol. 27, pp. 23- 30 ,(2011) , 10.1111/J.2042-7158.1975.TB09373.X
A. J. Buller, J. C. Eccles, Rosamond M. Eccles, Differentiation of fast and slow muscles in the cat hind limb. The Journal of Physiology. ,vol. 150, pp. 399- 416 ,(1960) , 10.1113/JPHYSIOL.1960.SP006394