QX 314 chloride

QX-314 blocks the potassium but not the sodium-dependent component of the opiate response in locus coeruleus neurons.[Pubmed:8205485]

Brain Res. 1994 Mar 14;639(2):320-4.

Opiates hyperpolarize locus coeruleus neurons by simultaneously opening K+ channels and turning off a resting Na(+)-dependent inward current. Intracellularly applied QX-314 reduced the opiate current to approximately 40% of the control and the residual current did not reverse near EK, suggesting lack of a significant K+ component. Replacement of Na+ virtually abolished the residual opiate response. Thus, QX-314 blocks the K+ but not the Na(+)-dependent component of the opiate-induced outward current in LC neurons.

The inhibition of sodium currents in myelinated nerve by quaternary derivatives of lidocaine.[Pubmed:4541340]

J Gen Physiol. 1973 Jul;62(1):37-57.

The inhibition of sodium currents by quaternary derivatives of lidocaine was studied in single myelinated nerve fibers. Membrane currents were diminished little by external quaternary lidocaine (QX). QX present in the axoplasm (<0.5 mM) inhibited sodium currents by more than 90%. Inhibition occurred as the sum of a constant, tonic phase and a variable, voltage-sensitive phase. The voltage-sensitive inhibition was favored by the application of membrane potential patterns which produce large depolarizations when sodium channels are open. Voltage-sensitive inhibition could be reversed by small depolarizations which opened sodium channels. One explanation of this observation is that QX molecules enter open sodium channels from the axoplasmic side and bind within the channels. The voltage dependence of the inhibition by QX suggests that the drug binds at a site which is about halfway down the electrical gradient from inside to outside of the sodium channel.