European Journal of Pharmacology 2008-11-19

Effects of three metabolites of propiverine on voltage-dependent L-type calcium currents in human atrial myocytes.

Melinda Wuest, Torsten Christ, Nicole Hiller, Manfred Braeter, Ursula Ravens

Index: Eur. J. Pharmacol. 598 , 94-98, (2008)

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Abstract

The non-selective muscarinic receptor antagonist propiverine impairs L-type Ca(2+) currents (I(Ca,L)) in human detrusor smooth muscle cells and atrial cardiomyocytes. Here, we have investigated the effects of three metabolites of propiverine on human cardiac I(Ca,L). Propiverine reduced I(Ca)(,L) with a -logIC(50) [M] value of 4.1, M-5 only showed minor effect on I(Ca)(,L) at high concentrations, M-6 did not influence I(Ca)(,L) at all. Like the parent compound M-14 also reduced I(Ca)(,L) (-logIC(50) [M]=4.6). We conclude, that propiverine and M-14 reduce cardiac I(Ca)(,L) at higher concentrations than in detrusor cells and therefore preferentially reduce I(Ca)(,L) in the urinary bladder than in the heart.