Inhibition of L-type calcium current by genistein, a tyrosine kinase inhibitor, in pregnant rat myometrial cells

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Abstract

Possible regulation of L-type Ca2+ channels by tyrosine kinase was examined in freshly isolated uterine smooth muscle cells obtained from late pregnant (18-19 day) rat, using whole-cell voltage clamp. Bath application of genistein, an inhibitor of tyrosine kinase, decreased L-type Ca2+ current (ICa(L)) dose-dependently. The maximal inhibition of ICa(L) was 46% and the concentration for half-maximal inhibition (IC50) was 50 μM (at a holding potential of -60 mV). The effect of genistein was reversible. Daidzein, an inactive analog of genistein, had no inhibitory effect on ka(L) at concentrations as high as 300 μM. The steady-state inactivation curve for ICa(L) was shifted to the left by genistein (15 mV at 100 μM), whereas the activation curve was not affected, suggesting that genistein exerts a voltage-dependent block. These results suggest that the L-type Ca2+ channels in myometrial cells may be modulated by endogenous tyrosine kinase, i.e., they are in a tonically stimulated state due to tyrosine kinase activity. This modulatory mechanism may play a role on the regulation of Ca2+ influx and uterine contraction during normal labor and preterm labor. © 1995.

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Kusaka, M., & Sperelakis, N. (1995). Inhibition of L-type calcium current by genistein, a tyrosine kinase inhibitor, in pregnant rat myometrial cells. BBA - Biomembranes, 1240(2), 196–200. https://doi.org/10.1016/0005-2736(95)00191-3

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