Effects of calmodulin antagonists on sodium-dependent high-affinity choline uptake.
Effects of calmodulin antagonists on sodium-dependent high-affinity choline uptake.
复制标题
钙调蛋白拮抗剂对钠依赖性高亲和力胆碱摄取的影响。
DOI：
10.1016/0006-8993(91)91006-m
复制
发表时间：
1991
期刊：
影响因子：
2.9
通讯作者：
Coyle,JT
中科院分区：
文献类型：
--
作者：
Yamada,K;Saltarelli,MD;Coyle,JT
通过[~ 3 H]HCH-3（[~ 3 H]hemicholinium-3）的特异性结合和高亲和力[~ 3 H]胆碱摄取来研究钙调素（CaM）拮抗剂对钠依赖性高亲和力胆碱摄取（SDHACU）的影响。钾去极化引起的显着的2倍增加[3 H]HCH-3的特异性结合在体外大鼠纹状体切片。钙调素拮抗剂，包括三氟拉嗪（TFP）、W-5、W-7、异丙嗪和氟哌啶醇，剂量依赖性地抑制钾去极化刺激的[3 HCH-3]结合，IC 50分别为20、40、70、30和48 μM。Scatchard分析表明，TFP的抑制作用是由于[~ 3 H]HCH-3结合的Bmax降低而Kd无变化。钾去极化也刺激高亲和力[3 H]胆碱摄取，10 μM TFP完全抑制。这些结果进行了讨论有关SDHACU的调节机制。
The effects of calmodulin (CaM) antagonists were investigated on the sodium-dependent high-affinity choline uptake (SDHACU) as assessed by the specific binding of [3H]hemicholinium-3 ([3H]HCh-3) and high-affinity [3H]choline uptake. Potassium depolarization caused a significant 2-fold increase in the specific binding of [3H]HCh-3 in slices of rat striatum in vitro. CaM antagonists, including trifluoperazine (TFP), W-5, W-7, promethazine and haloperidol, dose-dependently inhibited potassium depolarization-stimulated [3HCh-3 binding with IC50s of 20, 40, 70, 30 and 48 (μM), respectively. Scatchard analysis revealed that the inhibitory effect of TFP resulted from a decrease inBmaxbut no change inKdof [3H]HCh-3 binding. Potassium depolarization of slices also stimulated high-affinity [3H]choline uptake, which was completely inhibited by 10 μM TFP. These results are discussed in relation to the regulatory mechanisms of SDHACU.