氯胺酮而非氟烷对神经元5-羟色胺摄取的抑制作用涉及转运体对底物识别的破坏。

Inhibition of neuronal 5-HT uptake by ketamine, but not halothane, involves disruption of substrate recognition by the transporter.

作者信息

Martin D C, Introna R P, Aronstam R S

机构信息

Department of Anesthesiology, Medical College of Georgia, Augusta 30912.

出版信息

Neurosci Lett. 1990 Apr 20;112(1):99-103. doi: 10.1016/0304-3940(90)90329-8.

DOI:10.1016/0304-3940(90)90329-8

PMID:2143567

Abstract

The effects of halothane and ketamine on (1) serotonin (5-hydroxytryptamine; 5-HT) uptake and (2) paroxetine binding to the 5-HT transporter in neuronal membranes were determined in rat brain. Both anesthetics inhibited the uptake of [3H]5-HT by synaptosomes, but only ketamine affected binding of [3H]paroxetine to the 5-HT transporter. Saturation analysis indicated that ketamine inhibition of [3H]paroxetine binding was competitive (Ki = 18.8 microM). These results indicate that halothane and ketamine inhibit 5-HT transport by different mechanisms.

摘要

在大鼠脑中测定了氟烷和氯胺酮对（1）血清素（5-羟色胺；5-HT）摄取以及（2）帕罗西汀与神经元膜中5-HT转运体结合的影响。两种麻醉剂均抑制突触体对[3H]5-HT的摄取，但只有氯胺酮影响[3H]帕罗西汀与5-HT转运体的结合。饱和分析表明，氯胺酮对[3H]帕罗西汀结合的抑制是竞争性的（Ki = 18.8 microM）。这些结果表明，氟烷和氯胺酮通过不同机制抑制5-HT转运。