地尔硫䓬对大鼠中枢神经系统中[³H] - 乙酰胆碱释放的影响。

Effects of diltiazem on [3H]-acetylcholine release in rat central nervous system.

Tsuda K, Tsuda S, Masuyama Y, Goldstein M

Division of Cardiology, Wakayama Medical College, Japan.

Clin Exp Pharmacol Physiol. 1994 Jul;21(7):533-7. doi: 10.1111/j.1440-1681.1994.tb02552.x.

Abstract

In the present study, we examined the effects of a Ca2+ channel blocker, diltiazem, on [3H]-acetylcholine (ACh) release in the rat CNS. 2. Diltiazem inhibited the electrically stimulated [3H]-ACh release in a dose-related fashion striatal slices of Sprague-Dawley (SD) rats. The basal release of [3H]-ACh was not significantly affected by diltiazem except at a high concentration. 3. The stimulation-evoked [3H]-ACh release was not different between spontaneously hypertensive rats (SHR) and Wistar-Kyoto (WKY) rats. 4. The inhibitory effect of diltiazem on the stimulation-evoked [3H]-ACh release was significantly greater in SHR than in WKY rats. 5. The results show that diltiazem inhibited the stimulation-evoked ACh release in the rat CNS. The pronounced effect of diltiazem in SHR suggests that the inhibition of central cholinergic activity might contribute, at least partially, to the hypotensive mechanisms of the Ca2+ channel blocker.

摘要

在本研究中，我们检测了钙通道阻滞剂地尔硫䓬对大鼠中枢神经系统中[3H]-乙酰胆碱（ACh）释放的影响。2. 地尔硫䓬以剂量相关的方式抑制了Sprague-Dawley（SD）大鼠纹状体切片中电刺激诱发的[3H]-ACh释放。除高浓度外，地尔硫䓬对[3H]-ACh的基础释放无显著影响。3. 自发性高血压大鼠（SHR）和Wistar-Kyoto（WKY）大鼠之间，刺激诱发的[3H]-ACh释放没有差异。4. 地尔硫䓬对刺激诱发的[3H]-ACh释放的抑制作用在SHR中比在WKY大鼠中显著更大。5. 结果表明，地尔硫䓬抑制了大鼠中枢神经系统中刺激诱发的ACh释放。地尔硫䓬在SHR中的显著作用表明，抑制中枢胆碱能活性可能至少部分地促成了钙通道阻滞剂的降压机制。