Effects of local anaesthetics on the activity of the Na,K-ATPase of canine renal medulla.
Effects of local anaesthetics on the activity of the Na,K-ATPase of canine renal medulla.
复制标题
局麻药对犬肾髓质Na,K-ATP酶活性的影响。
DOI：
10.1006/phrs.1999.0547
复制
发表时间：
2000
影响因子：
9.3
通讯作者：
Farley,RA
中科院分区：
文献类型：
--
作者：
Kutchai,H;Geddis,LM;Farley,RA
本研究的目的是表征局部麻醉剂对Na，K-ATP酶活性的影响。在37 ° C和25°C下，在不存在和存在利多卡因、普鲁卡因、丁卡因、苯扎卡因、布比卡因、丙胺卡因和普鲁卡因酰胺的情况下，测定了犬肾髓质Na，K-ATP酶富集膜的ATP酶活性。在25 ° C和37°C下，除苯并咪唑外，所有这些局部麻醉剂均抑制犬肾髓质Na，K-ATP酶的活性。苯佐卡因在37°C下抑制Na，K-ATP酶活性，但在25°C下刺激活性。观察了利多卡因对Na+、K+刺激Na，K-ATP酶活性的影响。利多卡因使Na ~+和K ~+的表观K_（0.5）增加，使Na ~+和K ~+的Vmax值降低。利多卡因的IC 50值随着Na+和K+浓度的增加而增加。数据表明，利多卡因降低了Na，K-ATP酶对Na+和K+的亲和力，Na+或K+的结合降低了利多卡因作为Na，K-ATP酶抑制剂的效力。利多卡因显著降低Na，K-ATP酶对哇巴因的亲和力，但仅轻微减少哇巴因结合的最大量。未质子化的利多卡因显然是比质子化形式更有效的抑制剂。2000年学术出版社@p$hr
The purpose of this study is to characterize the effects of local anaesthetics on Na,K-ATPase activity. The ATPase activity of Na,K-ATPase-enriched membranes from canine renal medulla was determined in the absence and in the presence of lidocaine, procaine, tetracaine, benzocaine, bupivacaine, prilocaine, and procainamide at 37 and 25°C. All of these local anaesthetics, except benzocaine, inhibit the activity of the Na,K-ATPase of canine renal medulla at both 25 and 37°C. Benzocaine inhibits Na,K-ATPase activity at 37°C, but stimulates activity at 25°C. The influence of lidocaine on stimulation of Na,K-ATPase activity by Na+and K+was investigated. Lidocaine increases the apparentK0.5of the Na,K-ATPase for both Na+and K+and decreases the Vmaxvalues for both ions. IC50values for lidocaine increase with increasing concentrations of both Na+and K+. The data indicate that lidocaine diminishes the affinity of the Na,K-ATPase for Na+and K+and that binding of Na+or K+decreases the potency of lidocaine as an inhibitor of the Na,K-ATPase. Lidocaine markedly decreases the affinity of the Na,K-ATPase for ouabain, but only slightly diminishes the maximum amount of ouabain bound. Unprotonated lidocaine is apparently a more potent inhibitor than is the protonated form. 2000 Academic Press@p$hr