D. Busselberg et al., VOLTAGE-GATED CALCIUM-CHANNEL CURRENTS OF RAT DORSAL-ROOT GANGLION (DRG) CELLS ARE BLOCKED BY AL3+, Brain research, 622(1-2), 1993, pp. 163-168
The effects of the trivalent cation aluminum (Al3+) on voltage activat
ed calcium channel currents were examined. Al3+ blocks sustained and t
ransient components of voltage activated calcium channel currents of c
ultured rat dorsal root ganglion (DRG) cells. Currents were elicited b
y voltage jumps from -80 to 0 mV. The channel block was use dependent.
Steady state blockade occurred after 1 to 5 min, when opening the cha
nnel every 10 s. There was little or no recovery after washing. Thresh
old concentration was about 20 muM Al3+ and total blockade (> 80%) was
obtained at 200 muM Al3+; the IC50 was 83 muM and the Hill number was
around 3. The degree of blockade was pH dependent, and increased with
H+ concentration. The current-voltage relation frequently shifted to
depolarised voltages after applying Al3+. The degree of the shift was
a function of Al3+ concentration, but the magnitude differed from cell
to cell. In the effective concentration range (< 200 muM Al3+) the ef
fect was quite specific to voltage activated calcium channel currents.
Voltage activated potassium and sodium channels were reduced less tha
n 15% by 200 muM Al3+. We conclude that Al3+ is a potent and irreversi
ble blocker of voltage activated calcium channel currents in mammalian
neurons.