Naunyn-Schmiedebergs Archives of Pharmacology 2001-07-01

Dibenzylamine--a novel blocker of the voltage-dependent K+ current in myocardial mouse cells.

B Doepner, R Koopmann, A Knopp, H Hirche, K Benndorf

Index: Naunyn Schmiedebergs Arch. Pharmacol. 364(1) , 9-13, (2001)

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Abstract

Ventricular myocytes of the mouse ventricle were voltage clamped with a patch-clamp technique in the whole-cell configuration. At depolarizing voltage pulses, these myocytes develop a large voltage-dependent K+ outward current. Application of the drug dibenzylamine (DBA) to the bath solution blocked the voltage-dependent K+ current. The concentration/response relationship for the peak current at +40 mV indicates a 1:1 binding of the drug to the receptor with a concentration of half maximum effect of 43.1 micromol/l. The block did not require activation of the channels by depolarizing pulses. At concentrations causing partial block (25 micromol/l), the block was independent of voltage. At the same concentration, DBA completely blocked the slow component of the recovery from inactivation (-80 mV) whereas steady-state inactivation was not altered. It is concluded that DBA is a novel blocker of the voltage-dependent K+ current in mouse cardiac myocytes which preferentially affects the current component generating the slow recovery from inactivation.