A drawback of most local anaesthetics is their non-specific action. Their lipophilic nature permits them access to any neuron, where they indiscriminately block sodium channels in the membrane. A membrane-impermeant sodium channel blocker, QX-314, can be targeted to pain-sensing neurons. The authors exploited the specific expression of TRPV1 channels in pain-sensing neurons, the opening of which by capsaicin allows QX-314 access to the inside of the cell.
- Alexander M. Binshtok
- Bruce P. Bean
- Clifford J. Woolf