An affinity-modulating site on neuronal monoamine transport proteins
An affinity-modulating site on neuronal monoamine transport proteins
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DOI：
10.1111/j.1600-0773.1997.tb00396.x
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发表时间：
1997-04-01
期刊：
影响因子：
--
通讯作者：
Mellerup, ET
中科院分区：
文献类型：
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作者：
Plenge, P;Mellerup, ET
发现[H-3]nisoxetine、[H-3]GBR 12935和[H-3]西酞普兰分别从大鼠脑去甲肾上腺素、多巴胺和5-HT转运体的解离速率受几种药物的显著影响。舍曲林强烈减弱[H-3]尼索西汀从去甲肾上腺素转运体的解离速率，而西酞普兰强烈减弱[H-3]西酞普兰从5-HT转运体的解离速率。这两种药物的作用是立体特异性的。关于[H-3]GBR 12935与多巴胺转运蛋白的解离，鉴定了效力较低的亲和力调节药物。因此，所有三种神经元单胺转运蛋白可能具有特定的亲和力调节位点，其改变转运蛋白的功能，可能影响突触活动期间释放的单胺的再摄取。
The dissociation rates of [H-3]nisoxetine, [H-3]GBR 12935 and [H-3]citalopram from, respectively, the rat brain noradrenaline, dopamine and 5-HT transporters were found to be markedly affected by several drugs. Sertraline strongly attenuated the rate of dissociation of [H-3]nisoxetine from the noradrenaline transporter, while citaropram strongly attenuated that of [H-3]citalopram from the 5-HT transporter. The effects of both drugs were stereospecific. Less potent affinity-modulating drugs were identified with regards to [H-3]GBR 12935 dissociation from the dopamine transporter. All three neuronal monoamine transporters may thus have specific affinity-modulating sites which change the function of the transporters with possible implications for the reuptake of monoamines released during synaptic activity.