A SIMPLE METHOD TO DETERMINE THE RATIO OF CARDIAC TO VASCULAR β-RECEPTOR BLOCKADE IN THE RAT IN VIVO

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We have devised a simple method to determine the ratios of cardiac to vascular β-receptor blockage (C : V ratios) in normotensive rats anesthetized with pentobarbital, and applied it to six β-adrenergic blocking drugs (β-blockers). Mean blood pressure (BP) and heart rate (HR) were recorded. Isoproterenol (3 ng-100 μg/kg, i.v.) was cumulatively injected before and after the intravenous administration of β-blockers at two dose-levels. Thus shifts of the dose-response curves in BP and HR were observed. "In vivo pA_2" values were calculated in molar doses per kg by Schild plots. The C : V ratio was calculated as antilogarithm of the difference of the mean in vivo pA_2 value in HR from that in BP. Those of atenolol, bometolol, bunitrolol, pindolol, propranolol, and sotalol were 9.77,8.13,2.95,1.38,1.20,and 0.71,respectively.
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