Retigabine刺激人类KCNQ2 /第三通道bupivacaine的存在。

文章的细节

引用

复制到剪贴板

庞克,Friederich P

Retigabine刺激人类KCNQ2 /第三通道bupivacaine的存在。

麻醉学。2004年8月,101 (2):430 - 8。

PubMed ID

15277926 (在PubMed

]

文摘

背景:抑制KCNQ2 /第三通道可能会引起痉挛。bupivacaine这些通道的交互是未知的。的抗惊厥的retigabine激活KCNQ2 /第三通道和bupivacaine可能反向抑制行为。因此,钾通道的刺激可能构成一个新颖的方法来治疗当地anesthetic-induced发作。本研究的目的是描述bupivacaine影响KCNQ2 /第三通道并调查是否retigabine逆转的影响局部麻醉。方法:KCNQ2 /第三通道是暂时性的中国仓鼠卵巢细胞中表达。bupivacaine的影响和retigabine与膜片箝技术进行了研究。结果:Bupivacaine抑制KCNQ2 /第三通道浓度和可逆的方式。量效曲线被希尔方程(IC50 = 173 + / - 7 microm,希尔系数= 1.4 + / - 0.1,意味着+ / - SEM, n = 37)。抑制效果没有差异bupivacaine和levobupivacaine (42 + / - 4%, n = 7,与42 + / - 5%,n = 10; P > 0.05). Ropivacaine was four times less potent than bupivacaine. The inhibition of KCNQ2/Q3 channels by bupivacaine resulted in a significant and reversible depolarization of the membrane potential. Retigabine (300 nm-10 microm) reversed the inhibitory action of bupivacaine on KCNQ2/Q3 channels as well as the depolarization of the membrane potential. CONCLUSIONS: The anticonvulsant retigabine at nanomolar concentrations reverses the inhibitory effect of micromolar concentrations of bupivacaine. Our results allow the hypothesis that activation of KCNQ2/Q3 channels by retigabine may offer a novel therapeutic approach for the treatment of bupivacaine-induced seizures.

beplay体育安全吗DrugBank数据引用了这篇文章

药物

Ezogabine