(original) (raw)

TY - JOUR AU - Binshtok, Alexander M. AU - Bean, Bruce P. AU - Woolf, Clifford J. PY - 2007 DA - 2007/10/01 TI - Inhibition of nociceptors by TRPV1-mediated entry of impermeant sodium channel blockers JO - Nature SP - 607 EP - 610 VL - 449 IS - 7162 AB - The snag with most local anaesthetics is their lack of specificity. They are lipophilic, so can enter virtually any neuron, where they indiscriminately block sodium channels in the membrane. A way of blocking the activity of specific pain-sensing neurons without affecting other sensory or motor neurons could be used to create a more targeted form of local anaesthesia, and that is the prospect held out by Binshtok et al. in this issue. They report that the lidocaine derivative QX-314 can be targeted to pain-sensing neurons. Normally QX-314 can't cross the cell membrane. But antipain specificity is ensured by allowing it to enter via the TRPV1 channel, a capsaicin receptor found only in pain-sensing neurons. Co-application of QX-314 and capsaicin in rats blocked mechanical and thermal pain, inducing local anaesthesia, without the paralysis seen in 'normal' lidocaine anaesthesia. SN - 1476-4687 UR - https://doi.org/10.1038/nature06191 DO - 10.1038/nature06191 ID - Binshtok2007 ER -