24003-58-5 N-乙基利多卡因溴化物

• 生物活性 QX-314 bromide 是一种膜不渗透的钠离子通道永久性电荷阻滞剂。
• 靶点 sodium channel
• 体外研究 QX-314 bromide exerts biphasic effects on transient receptor potential vanilloid subtype 1 channels (TRPV1) in vitro . QX-314 bromide (1–60 mM) directly activates TRPV1 in a concentration-dependent manner. QX-314 bromide (≥ 30 mM) produces oocyte membrane blackening and cell death . QX-314 bromide inhibits calcium currents in hippocampal CA1 pyramidal neurons intracellular, and the low-threshold (T-type) Ca 2+ currents are on average < 10% of control amplitude . QX-314 bromide shifts the current-voltage relationships (I-Vs) in the positive voltage direction due to the presence of intracellular Br- .
• 体内研究 QX-314 bromide (1.6 mg/kg; i.c.) abolishes responses to noxious mechanical and thermal stimuli without motor or tactile deficits when co-treatment with capsaicin. Animal Model: Male Sprague-Dawley rats (250-290 g) Dosage: 1.6 mg/kg Administration: Intracutaneous injection Result: Abolished responses to noxious mechanical and thermal stimuli without motor or tactile deficits when co-treatment with capsaicin.

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