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Electrophysiological effects of amosulalol a new alpha adrenoceptor and beta adrenoceptor blocker in isolated rabbit papillary muscles


, : Electrophysiological effects of amosulalol a new alpha adrenoceptor and beta adrenoceptor blocker in isolated rabbit papillary muscles. European Journal of Pharmacology 125(3): 411-420

The electrophysiological effects of amosulalol, a newly developed .alpha.- and .beta.-adrenoceptor blocking agent, were examined and compared with those of labetalol, prazosin and propranolol in isolated rabbit papillary muscles by means of standard microelectrode techniques. Amosulalol above 3 .mu.M produced a concentration-dependent decrease in the maximum rate of depolarization .ovrhdot.Vmax and an increase in action potential duration (APD). Labetalol and prazosin produced a similar APD prolongation, and .ovrhdot.Vmax was depressed by all these drugs in a concentration-dependent manner. The depressant action of these drugs on .ovrhdot.Vmax was enhanced by increasing the stimulation rate from 0.25 to 2.0 Hz. In the presence of these drugs the .ovrhdot.Vmax declined exponentially to a new plateau level (rate-dependent block) and the onset of the rate dependent block for amosulalol at 1 Hz was similar to that for labetalol and propranolol, and faster than that for prazosin. The time constants of the recovery from rate-dependent block for amosulalol, labetalol and prazosin were considerably slower than that for propranolol. These results suggest that amosulalol possesses class I and III antiarrhythmic properties and the recovery from the rate-dependent block of .ovrhdot.Vmax is relatively slow with this drug.

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