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[丁螺环酮及其樟脑酰亚胺类似物对5-羟色胺能效应的抑制作用的不同机制]

[The different mechanism of the inhibition by buspirone and its camphorimide analogs of 5-HT3-serotoninergic effects].

作者信息

Kharin N A, Abramets I I, Komissarov I V, Samoĭlovich I M

出版信息

Biull Eksp Biol Med. 1993 Aug;116(8):167-9.

PMID:7903873
Abstract

Serotonin evokes the depolarization and the membrane resistance lowering of rat dorsal root ganglion neurones when a K(+)--conductance of the neuronal membranes is blocked by Cs+ intracellular injection. These 5-HT3-effects ere diminished and removed by preliminary superfusion of the ganglions with saline containing busperone or its structural analogues. The effects of camphorimide analogues of buspirone (campirone, pyricapirone) could not be reproduced in case of the protein kinase A blockade by tolbutamide (100 microM/l). It is suggested that camphorimide analogues are the 5-HT3 receptor blockers while busperone and ipsapirone modulate 5-HT3 receptor affinity by decreasing the protein kinase A activity.

摘要

当通过细胞内注射Cs⁺阻断神经元膜的K⁺电导时,血清素可引起大鼠背根神经节神经元的去极化和膜电阻降低。在用含有丁螺环酮或其结构类似物的盐水对神经节进行预灌流后,这些5-HT₃效应减弱并消除。在甲苯磺丁脲(100微摩尔/升)阻断蛋白激酶A的情况下,丁螺环酮的樟脑酰亚胺类似物(坎皮隆、吡咯卡哌隆)的效应无法重现。提示樟脑酰亚胺类似物是5-HT₃受体阻滞剂,而丁螺环酮和伊沙匹隆通过降低蛋白激酶A活性来调节5-HT₃受体亲和力。

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