产品描述:
QX-314 is a membrane-impermeant lidocaine derivative that selectively blocks sodium channels on nociceptive neurons when delivered intracellularly via the TRPV1 channel, but is reportedly ineffective with extracellular application.{15625} When supplied in combination with 1 µM capsaicin, a TRPV1 receptor agonist, 5 mM QX-314 blocks 98% of sodium current in voltage-clamped nociceptive DRG neurons.{15625} QX-314 elicits a long-lasting decrease in the response to painful mechanical and thermal stimuli without imparting the motor deficits (e.g., numbness, paralysis) associated with many conventional local anesthetics.{15625} At concentrations ranging from 10-70 mM, peripheral application of QX-314 dose-dependently produces robust local anesthesia with slow onset in the guinea pig intradermal wheal assay, the murine tail-flick test, and the murine sciatic nerve blockade model.{16613} However, injection of 0.5-30 mM QX-314 in the lumbar intrathecal space produces neurotoxicity and death in mice.{16615}