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<p>Large-pore ion channels present a window of opportunity for cell-specific intracellular drug delivery. Here, we demonstrate that the capsaicin receptor, TRPV1, can be used for delivery of the membrane impermeant lidocaine derivative QX-314 into neurons in the brain in vivo by using drug-induced hyperlocomotion as a behavioral readout and we validated our findings with ex vivo electrophysiological recordings. Our studies present evidence that this strategy can be used to deliver membrane impermeant compounds in the brain.</p>

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Leveraging TRPV1 for intracellular delivery of membrane impermeant compounds in the brain

  • 期刊论文

  • 出版模式：

    开放获取

  • 发表日期：

    2025年12月12日

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  • José C. Zepeda,
  • Loren D. Peeters,
  • Pragnya S. Adapa,
  • Beimnet B. Kassaye,
  • Brad A. Grueter

摘要

Large-pore ion channels present a window of opportunity for cell-specific intracellular drug delivery. Here, we demonstrate that the capsaicin receptor, TRPV1, can be used for delivery of the membrane impermeant lidocaine derivative QX-314 into neurons in the brain in vivo by using drug-induced hyperlocomotion as a behavioral readout and we validated our findings with ex vivo electrophysiological recordings. Our studies present evidence that this strategy can be used to deliver membrane impermeant compounds in the brain.