Local anaesthetics potentiate GABA-mediated Cl currents by inhibiting GABA uptake

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A two-electrode voltage clamp was used to examine the effects of the local anaesthetics (LAs) lidocaine, tetra- caine and bupivacaine, and the meta-isomer of lidocaine (LL33), on the γ-aminobutyric acid (GABA)-gated Cl channel in the crayfish stretch receptor neurone. The voltage-induced current changes were recorded while exposing the neurone to GABA in saline containing different LAs. All LAs enhanced the voltage-induced Cl current equivalent to a shift of the conductance vs GABA curve towards lower concentrations. The mechanism of the facilitation of GABA-induced conductance was found to be mainly a block of the GABA uptake in the stretch receptor neurone. Tetracaine, and to a lesser extent LL33, also seem to affect directly the GABA/receptor Cl/channel complex resulting in an increased conductance of the channel.

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