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Targeting of sodium channel blockers into nociceptors to produce long-duration analgesia: a systematic study and review.

Roberson DP, Binshtok AM, Blasl F, Bean BP, Woolf CJ.

Br J Pharmacol. 2011 Sep;164(1):48-58. doi: 10.1111/j.1476-5381.2011.01391.x. Review.


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

Binshtok AM, Bean BP, Woolf CJ.

Nature. 2007 Oct 4;449(7162):607-10.


Acid solution is a suitable medium for introducing QX-314 into nociceptors through TRPV1 channels to produce sensory-specific analgesic effects.

Liu H, Zhang HX, Hou HY, Lu XF, Wei JQ, Wang CG, Zhang LC, Zeng YM, Wu YP, Cao JL.

PLoS One. 2011;6(12):e29395. doi: 10.1371/journal.pone.0029395.


Coapplication of lidocaine and the permanently charged sodium channel blocker QX-314 produces a long-lasting nociceptive blockade in rodents.

Binshtok AM, Gerner P, Oh SB, Puopolo M, Suzuki S, Roberson DP, Herbert T, Wang CF, Kim D, Chung G, Mitani AA, Wang GK, Bean BP, Woolf CJ.

Anesthesiology. 2009 Jul;111(1):127-37. doi: 10.1097/ALN.0b013e3181a915e7.


Emulsified isoflurane enhances thermal transient receptor potential vanilloid-1 channel activation-mediated sensory/nociceptive blockade by QX-314.

Zhou C, Liang P, Liu J, Zhang W, Liao D, Chen Y, Chen X, Li T.

Anesthesiology. 2014 Aug;121(2):280-9. doi: 10.1097/ALN.0000000000000236.


Quaternary Lidocaine Derivative QX-314 Activates and Permeates Human TRPV1 and TRPA1 to Produce Inhibition of Sodium Channels and Cytotoxicity.

Stueber T, Eberhardt MJ, Hadamitzky C, Jangra A, Schenk S, Dick F, Stoetzer C, Kistner K, Reeh PW, Binshtok AM, Leffler A.

Anesthesiology. 2016 May;124(5):1153-65. doi: 10.1097/ALN.0000000000001050.


Bupivacaine-induced cellular entry of QX-314 and its contribution to differential nerve block.

Brenneis C, Kistner K, Puopolo M, Jo S, Roberson D, Sisignano M, Segal D, Cobos EJ, Wainger BJ, Labocha S, Ferreirós N, von Hehn C, Tran J, Geisslinger G, Reeh PW, Bean BP, Woolf CJ.

Br J Pharmacol. 2014 Jan;171(2):438-51. doi: 10.1111/bph.12466.


Selectively targeting pain in the trigeminal system.

Kim HY, Kim K, Li HY, Chung G, Park CK, Kim JS, Jung SJ, Lee MK, Ahn DK, Hwang SJ, Kang Y, Binshtok AM, Bean BP, Woolf CJ, Oh SB.

Pain. 2010 Jul;150(1):29-40. doi: 10.1016/j.pain.2010.02.016.


Permeation and block of TRPV1 channels by the cationic lidocaine derivative QX-314.

Puopolo M, Binshtok AM, Yao GL, Oh SB, Woolf CJ, Bean BP.

J Neurophysiol. 2013 Apr;109(7):1704-12. doi: 10.1152/jn.00012.2013.


Expression of TRPV1 channels after nerve injury provides an essential delivery tool for neuropathic pain attenuation.

Zakir HM, Mostafeezur RM, Suzuki A, Hitomi S, Suzuki I, Maeda T, Seo K, Yamada Y, Yamamura K, Lev S, Binshtok AM, Iwata K, Kitagawa J.

PLoS One. 2012;7(9):e44023. doi: 10.1371/journal.pone.0044023.


The quaternary lidocaine derivative, QX-314, exerts biphasic effects on transient receptor potential vanilloid subtype 1 channels in vitro.

Rivera-Acevedo RE, Pless SA, Ahern CA, Schwarz SK.

Anesthesiology. 2011 Jun;114(6):1425-34. doi: 10.1097/ALN.0b013e318216ea0c. Erratum in: Anesthesiology. 2015 Aug;123(2):492.


Phenotyping the function of TRPV1-expressing sensory neurons by targeted axonal silencing.

Brenneis C, Kistner K, Puopolo M, Segal D, Roberson D, Sisignano M, Labocha S, Ferreirós N, Strominger A, Cobos EJ, Ghasemlou N, Geisslinger G, Reeh PW, Bean BP, Woolf CJ.

J Neurosci. 2013 Jan 2;33(1):315-26. doi: 10.1523/JNEUROSCI.2804-12.2013.


Prolonged analgesic response of cornea to topical resiniferatoxin, a potent TRPV1 agonist.

Bates BD, Mitchell K, Keller JM, Chan CC, Swaim WD, Yaskovich R, Mannes AJ, Iadarola MJ.

Pain. 2010 Jun;149(3):522-8. doi: 10.1016/j.pain.2010.03.024.


Nociceptor-selective peripheral nerve block induces delayed mechanical hypersensitivity and neurotoxicity in rats.

Peters CM, Ririe D, Houle TT, Aschenbrenner CA, Eisenach JC.

Anesthesiology. 2014 Apr;120(4):976-86. doi: 10.1097/ALN.0000000000000088.


External QX-314 inhibits evoked cranial primary afferent synaptic transmission independent of TRPV1.

Hofmann ME, Largent-Milnes TM, Fawley JA, Andresen MC.

J Neurophysiol. 2014 Dec 1;112(11):2697-706. doi: 10.1152/jn.00316.2014.


EN3427: a novel cationic aminoindane with long-acting local anesthetic properties.

Banerjee M, Baranwal A, Saha S, Saha A, Priestley T.

Anesth Analg. 2015 Apr;120(4):941-9. doi: 10.1213/ANE.0000000000000629.


Neuroscience: a local route to pain relief.

McCleskey EW.

Nature. 2007 Oct 4;449(7162):545-6. No abstract available.


Duration and local toxicity of sciatic nerve blockade with coinjected site 1 sodium-channel blockers and quaternary lidocaine derivatives.

Shankarappa SA, Sagie I, Tsui JH, Chiang HH, Stefanescu C, Zurakowski D, Kohane DS.

Reg Anesth Pain Med. 2012 Sep-Oct;37(5):483-9. doi: 10.1097/AAP.0b013e31826125b3.


The quaternary lidocaine derivative QX-314 produces long-lasting intravenous regional anesthesia in rats.

Zhao Y, Zhou C, Liu J, Liang P, Liao D, Chen Y, Chen X.

PLoS One. 2014 Jun 16;9(6):e99704. doi: 10.1371/journal.pone.0099704.


Differential effects of TRPV channel block on polymodal activation of rat cutaneous nociceptors in vitro.

St Pierre M, Reeh PW, Zimmermann K.

Exp Brain Res. 2009 Jun;196(1):31-44. doi: 10.1007/s00221-009-1808-3. Review.

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