Inhibition of the Na,K-ATPase of canine renal medulla by several local anesthetics.
Inhibition of the Na,K-ATPase of canine renal medulla by several local anesthetics.
复制标题
几种局麻药对犬肾髓质 Na,K-ATP 酶的抑制。
DOI：
10.1006/phrs.2001.0803
复制
发表时间：
2001
影响因子：
9.3
通讯作者：
Geddis,LM
中科院分区：
文献类型：
--
作者：
Kutchai,H;Geddis,LM
在无局部麻醉剂和存在普鲁卡因、氯普鲁卡因、布比卡因、甲哌卡因、利多卡因和利多卡因的两种季铵衍生物（QX-222和QX-314）的情况下，在37 ℃下测定了犬肾髓质Na，K-ATP酶富集膜的ATP酶活性。氯普鲁卡因（IC 50 = 13 mM）的效力略高于普鲁卡因（IC 50 = 17.7 mM）。布比卡因（IC 50 = 6.7 mM）比其同类物甲哌卡因（IC 50> 10 mM，溶解度极限）更有效。QX-222（IC 50> 600 mM）和QX-314（IC 50 = 132 mM）的效力低于利多卡因（IC 50 = 30.4 mM）。这项研究支持的解释，不带电形式的局部麻醉剂是更有效的抑制剂的Na，K-ATP酶活性比阳离子形式。
The ATPase activity of Na,K-ATPase-enriched membranes from canine renal medulla was determined in the absence of local anesthetic and in the presence of procaine, chloroprocaine, bupivacaine, mepivacaine, lidocaine, and two quaternary derivatives of lidocaine (QX-222 and QX-314) at 37∘C. Chloroprocaine (IC50= 13 mM) had slightly greater potency than procaine (IC50= 17.7 mM). Bupivacaine (IC50= 6.7 mM) was more potent than its congener mepivacaine (IC50> 10 mM, the solubility limit). QX-222 (IC50> 600 mM) and QX-314 (IC50= 132 mM) had less potency than lidocaine (IC50= 30.4 mM). This study supports the interpretation that the uncharged forms of local anesthetics are much more potent inhibitors of Na,K-ATPase activity than the cationic forms.