Characterization of [(125)~I]RTI-121 binding to dopamine transporter in vitro

被引：0
|
作者：
陈念航 [1 ]
丁建花 [1 ]
王幼林 [1 ]
机构：
[1] 南京医科大学药理教研室
来源：
Acta Pharmacologica Sinica | 1997年 / 02期
关键词：
多巴胺; RTI-121结合; 纹状体; 突触体; 莨菪烷类;
D O I：
暂无
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学科分类号：
摘要：
研究［１２５Ｉ］ＲＴＩ１２１与中枢多巴胺转运体（ＤＡＴ）在体外结合的特征．方法：在人工脑脊液（ＡＣＳＦ）中，３７℃下，用［１２５Ｉ］ＲＴＩ１２１标记大鼠纹状体突触体膜上ＤＡＴ．结果：［１２５Ｉ］ＲＴＩ１２１结合于３ｍｉｎ内达到平衡并稳定在峰值至少９ｍｉｎ．动力学研究、饱和分析和竞争抑制实验均提示［１２５Ｉ］ＲＴＩ１２１结合到一个位点上．ＤＡＴ阻断药可卡因、ＧＢＲ１２９３５和ＢＴＣＰ以及ＤＡＴ底物多巴胺和苯丙胺均竞争性抑制［１２５Ｉ］ＲＴＩ１２１结合．与ＮａＰｈｏｓＫＣｌＮａＣｌ缓冲液比较，含Ｃａ２＋和Ｍｇ２＋的ＡＣＳＦ显著增加阻断药的ＩＣ５０，而对底物的ＩＣ５０影响较小．Ｄ２受体配基培高利特、ｑｕｉｎｐｉｒｏｌｅ、舒必利和左旋千金藤立定对［１２５Ｉ］ＲＴＩ１２１结合无直接作用．结论：生理性条件下［１２５Ｉ］ＲＴＩ１２１结合满足ＤＡＴ结合分析所需的基本标准．
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页码：20 / 25
页数：6
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