锝99 m标记1 - (4-fluorobenzyl) 4 - (2-mercapto-2-methyl-4-azapentyl) 4 - (2-mercapto-2-methylprop ylamino)哌啶和碘- 123 metaiodobenzylguanidine为研究心脏肾上腺素的功能:一个比较的吸收特征和新生儿心脏细胞,血管平滑肌细胞和老鼠的调查。

文章的细节

引用 复制到剪贴板

朔伊尔Samnick年代,C,芒克年代,El-Gibaly,门格尔医学博士Kirsch厘米

诊断医学杂志。2004;31(4):511 - 22所示。

PubMed ID

15093822 (在PubMed

]

文摘

在发展中锝99 m -体内放射性配体为基础的研究心脏肾上腺素能神经元,我们比较的吸收特征(99米)Tc-labeled 1 - (4-fluorobenzyl) 4 - (2-mercapto-2-methyl-4-azapentyl) 4 - (2-mercapto-2-methylprop ylamino)哌啶((99)Tc-FBPBAT)与临床建立meta -[(123)我]iodobenzylguanidine ((123) I-MIBG)在大鼠血管平滑肌细胞和新生儿心脏细胞。此外,心脏和extracardiac吸收放射性药物评估在完整的老鼠和老鼠使用不同的α-和beta-adrenoceptor药物和肾上腺素的再摄取阻断剂。(99米)的吸收Tc-FBPBAT和(123)I-MIBG为血管平滑肌细胞和新生儿心脏细胞快速;超过85%的放射性物质积累进入细胞内发生第一次3分钟。放射性摄取后60分钟孵化在37摄氏度(pH值7.4)从15%变化到65%的总活动每百万细胞加载。在所有情况下,(99米)Tc-FBPBAT显示吸收越高,相对于(123)I-MIBG,在任何给定的细胞浓度。(99米)的细胞吸收Tc-FBPBAT是4度摄氏20度低于37度C .相比之下,(123)I-MIBG吸收只是轻微的温度依赖性。抑制实验证实(123)的细胞吸收I-MIBG uptake-I介导的载体,而α(1)-和β(1)-adrenoceptors主要是参与(99米)的吸收Tc-FBPBAT心血管组织。Biodistribution对老鼠的研究表明(99米)Tc-FBPBAT积累在静脉注射后心肌。放射性在老鼠心脏达2.32%和1.91%的注射剂量每克15岁和60分钟接受,而3.10%和2.21%注射剂量每克组织(% ID / g)与(123)I-MIBG实验,分别。 Prazosin, urapidil, and metoprolol were as effective as treatment with other adrenergic drugs in lowering cardiac uptake of (99m)Tc-FBPBAT. Uptake reduction was more pronounced in myocardium than in other adrenergic-rich organs, including the lung, spleen, kidney, and adrenals, suggesting that the (99m)Tc-FBPBAT uptake in myocardium specifically reflects a high degree of alpha(1)/beta(1)-receptor binding to cardiac adrenergic neurons. In comparison, reduction of cardiac and pulmonary uptake of (123)I-MIBG was effective after pretreatment of rats with desipramine and reserpine, confirming distinct neuronal binding sites for (99m)Tc-FBPBAT and (123)I-MIBG. (99m)Tc-FBPBAT was excreted via urine and to a lower degree via feces. Urine analysis 6 hours p.i. revealed that more than 40% of the total excreted radioactivity was unmetabolized (99m)Tc-FBPBAT. In conclusion, the uptake of (99m)Tc-FBPBAT in rat myocardium specifically reflects binding to cardiac adrenergic neurons. The (99m)Tc-FBPBAT uptake appears to be predominantly mediated via the alpha(1)/beta(1)-adrenoceptor pathway. These data indicate that (99m)Tc-FBPBAT, like (123)I-MIBG, may be suitable for mapping cardiac adrenergic innervation by SPET, especially for alpha(1)/beta(1)-adrenoceptors as target in numerous heart diseases.

DrugBank数据引用了这篇文章

药物靶点

药物	目标	类	生物	药理作用	行动
去郁敏	beta 1肾上腺素能受体	蛋白质	人类	未知的	其他	细节