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COMPARISON OF THE ACTIONS OF ACEBUTOLOL, PRACTOLOL AND PROPRANOLOL ON CALCIUM TRANSPORT BY HEART MICROSOMES AND MITOCHONDRIA

1976; Wiley; Volume: 57; Issue: 2 Linguagem: Inglês

10.1111/j.1476-5381.1976.tb07470.x

1476-5381

Naranjan S. Dhalla, S.L. LEE,

Cardiac electrophysiology and arrhythmias

The effects of acebutolol, practolol and propranolol (0.5‐3 m m ) on calcium uptake, calcium binding and ATPase activities of the rabbit and rat heart microsomal and mitochondrial fractions were investigated. Dose‐response and time course experiments revealed that propranolol greatly inhibited microsomal and mitochondrial calcium uptake whereas both acebutolol and practolol showed slight depressant effects. The ATPase activities of microsomal and mitochondrial fractions were decreased by acebutolol, practolol and propranolol; however, the latter agent was more effective than the other two. The inhibitory effects of acebutolol, practolol and propranolol on mitochondria and microsomes were not antagonized by adrenaline. Propranolol decreased calcium binding by the microsomal fraction only, whereas acebutolol and practolol had no effect on microsomal or mitochondrial calcium binding. The sensitivity of the rabbit heart subcellular fractions to the β‐adrenoceptor blocking drugs was similar to that of the rat heart; however, the calcium uptake and ATPase activities of microsomes were more sensitive to propranolol than mitochondria in both species. Perfusion of rat hearts with 0.2‐1 m m propranolol decreased contractile force, and microsomal and mitochondrial fractions obtained from these hearts accumulated less calcium in comparison to the control. On the other hand, acebutolol and practolol (0.2‐1 n m ) had no appreciable effects on contractile force or subcellular fractions under similar conditions. The negative inotropic effect of propranolol may partly be due to its inhibitory actions on calcium transport by subcellular organelles of the myocardium; the depressant action of propranolol on calcium transport is unlikely to be due to its β‐adrenoceptor blocking property.