Inhibition of nociceptors by TRPV1-mediated entry of impermeant sodium channel blockers

Alexander M. Binshtok, Bruce P. Bean () and Clifford J. Woolf
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Alexander M. Binshtok: Massachusetts General Hospital and Harvard Medical School, Charlestown, Massachusetts 02129, USA
Bruce P. Bean: Harvard Medical School, 220 Longwood Avenue, Boston, Massachusetts 02115, USA
Clifford J. Woolf: Massachusetts General Hospital and Harvard Medical School, Charlestown, Massachusetts 02129, USA

Nature, 2007, vol. 449, issue 7162, 607-610

Abstract: Hit where it hurts 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.

Date: 2007
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DOI: 10.1038/nature06191

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