快速检测SPECT altropane:帕金森病的多巴胺转运蛋白的选择性配体。

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费奇曼AJ,当时求职中介Bonab AA, Babich JW,帕默EP, Alpert NM, Elmaleh博士,卡拉汉RJ,巴罗SA Meltzer PC,格雷厄姆•W•汉森RN,马德拉斯BK

快速检测SPECT altropane:帕金森病的多巴胺转运蛋白的选择性配体。

突触。1998年6月29日(2):128 - 41。

PubMed ID

9593103 (在PubMed

]

文摘

越来越多的证据表明,多巴胺(DA)运输密度下降帕金森病(PD)。2 beta-carbomethoxy-3beta (4-fluorophenyl) - n - (1-iodoprop-1-en 3-yl) nortropane (IACFT Altropane)是一个可卡因模拟高亲和力和选择性在纹状体多巴胺转运体(DAT)的网站。在这项研究中,单光子发射计算机断层扫描(SPECT) [123 i] altropane是用来测量DAT密度在七个健康志愿者(五个男性,年龄37 - 75和两个女性,年龄在26岁至39岁)和八个男性帕金森氏症患者(年龄14 - 79、Hoehn和Yahr阶段:1.5 - 3 (n = 5)和4 - (n = 3))。动态SPECT图像和动脉血液样本获得超过1.5 2小时和等离子体辐射分析色谱得到的代谢物纠正动脉输入功能。绑定的潜在(BP, B 'max / KD)纹状体(Str) DAT网站是由两种方法计算使用枕叶皮质区(Occ)作为参考。在第一种方法,组织时间曲线(TAC)和代谢物纠正动脉输入功能是由一个线性图形分析方法为可逆的开发受体配体。在第二种方法中,表达式(Str (TAC)——Occ (TAC))是安装在一个γ变量函数和最大值除以Occ (TAC)在同一时间被用来估计英国石油公司。在五的PD患者,SPECT数据比较与宠物的结果[18 f] 6-fluoro多巴(FD-PET)。等离子体分析表明[123 i] altropane迅速转化为极性代谢物。在健康志愿者SPECT图像显示[123 i] altropane迅速积累,有选择地在纹状体和获得优质图像后1小时内注入。 Both methods of analysis revealed a 7.6%/decade reduction in BP and average striatal values (corrected to age 25) were 1.83 +/- 0.22 and 2.09 +/- 0.20 by methods 1 and 2. In all the PD patients, striatal accumulation was markedly reduced and the pattern of loss was similar to that reported for DA; most profound in the posterior putamen with relative sparing of the caudate nuclei. A comparable pattern was observed with FD-PET. For total striatum, age-corrected BP was significantly (P < 0.001) reduced; 0.83 +/- 0.06 (method 1), 0.84 +/- 0.07 (method 2). BPs measured by the two methods were remarkably similar and highly correlated r2 = 0.88, (P < 0.001). These results indicate that [123I]altropane is an excellent SPECT ligand for imaging the DAT/DA neurons in human brain. The high selectivity and rapid striatal accumulation of the ligand allows for accurate quantitation of DAT sites in less than 2 hr. The results further demonstrate that [123I]altropane is an effective marker for PD.

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药物

Altropane