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Journal of Pharmacology And Experimental Therapeutics, Vol. 189, Issue 3, 616-625, 1974
Copyright © 1974 by American Society for Pharmacology and Experimental Therapeutics

STUDIES ON THE EFFECTS OF ENANTIOMERS OF SOTERENOL, TRIMETOQUINOL AND SALBUTAMOL ON BETA ADRENERGIC RECEPTORS OF ISOLATED GUINEA-PIG ATRIA AND TRACHEA

C. K. Buckner 1 and P. Abel 1

1 School of Pharmacy, The University of Wisconsin, Madison, Wisconsin

Beta adrenergic receptors of guinea-pig atria and trachea were investigated with enantiomers of tissue selective agonists: soterenol, trimetoquinol and salbutamol. If the receptors of these two tissues are different, the ratio of potencies between enantiomers of the agonists should reflect the unique asymmetries of the receptors. From atria and trachea, enantiomeric potency differences (in log units) are: for soterenol, 1.86 and 2.19; for trimetoquinol, 1.61 and 1.56 and for salbutamol, 1.86 and 2.19, respectively. From both tissues, the values for each pair of isomers are identical. Analysis of tissue selectivity from potency values reveals that (—)-isomers of soterenol, trimetoquinol and salbutamol, are, respectively, 3.3-, 9- and 24-fold more potent in trachea than atria. However, when compared to (—)-isoproterenol on a relative potency basis in each tissue, only salbutamol is shown to have any degree of selectivity for trachea. When relative activities are compared from atria, soterenol and salbutamol appear as "partial agonists" while trimetoquinol produces about 90% of the maximum effect of isoproterenol. All agonists produce the same maximum effects in trachea. In atria, sotalol blocks the effects of the isomers of soterenol to a greater extent than it blocks the effects of isoproterenol and the isomers of trimetoquinol. It is suggested that factors other than ligand binding modes on the receptor could account for these observations. The data support previous suggestions that agonist binding sites on beta receptors of guinea-pig atria and trachea may be similar. Tissue selectivity of agonists may reflect different requirements for access to receptors or intrinsic activities between atria and trachea.

Submitted on May 29, 1973
Accepted on January 14, 1974




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