Most local anesthetics act by abolishing voltage gated sodium channel currents indiscriminately in all populations of neurons. Selective analgesia through TRPV1-mediated entry of a cationic lidocaine derivative, QX314, was recently reported.1 CAY10568 is a physically smaller, less hydrophobic version of QX314 designed to be even more permeable to the TRPV1 ion channel when activated by agonists such as capsaicin and N-oleoyl dopamine. CAY10568 when given in combination with suitable TRPV1 agonists should produce selective blockade of the pain response while leaving motor, touch, and proprioception intact.
1
Binshtok, A.M., Bean, B.P., and Woolf, C.J. Inhibition of nociceptors by TRPV1-mediated entry of impermeant sodium channel blockers. Nature449607-610(2007).
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[I-].O=C(Nc1ccccc1)C[N+](C)(C)C
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Binshtok, A.M., Bean, B.P., and Woolf, C.J. Inhibition of nociceptors by TRPV1-mediated entry of impermeant sodium channel blockers. Nature449607-610(2007).
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