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Lead-induced blockade of kainate-sensitive receptor channels

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Abstract

The effects of bivalent lead on ion channels activated by kainate and α-amino-3-hydroxy-5-methyl-4-isoxazolpropionate (AMPA) were studied using Xenopus oocytes microinjected with mRNA from rat brain. Lead reduced kainate-induced membrane currents in a reversible and dose-dependent manner, without affecting membrane currents induced by AMPA. Lead decreased the kainate currents with a concentration of 0.1 μmol/l to 0.93 ± 0.01 and with a concentration of 100 μmol/l to 0.41 ± 0.04 of the control values. The blocking effect of lead on kainate responses was voltage dependent. The inhibition was strongest at - 90 mV to - 70 mV and became weaker at more positive membrane potentials. The effect of lead on the kainate-induced membrane currents remained unchanged when the concentration of kainate was increased. Hence lead probably represents a noncompetitive channel-blocking agent for non-N-methyl-d-aspartate (NMDA) receptor channels activated by kainate.

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Mußhoff, U., Madeja, M., Binding, N. et al. Lead-induced blockade of kainate-sensitive receptor channels. Naunyn-Schmiedeberg's Arch Pharmacol 353, 42–45 (1995). https://doi.org/10.1007/BF00168914

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  • DOI: https://doi.org/10.1007/BF00168914

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