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一些影响N-异丙基对碘安非他明(IAMP)在脑内和脑外蓄积的因素。

Some factors affecting the cerebral and extracerebral accumulation of N-isopropyl-p-iodo-amphetamine (IAMP).

作者信息

Som P, Oster Z H, Yamamoto K, Meinken G E, Srivastava S C, Yonekura Y, Ebner S A, Atkins H L, Brill A B, Fawwaz R A

出版信息

Int J Nucl Med Biol. 1985;12(3):185-96. doi: 10.1016/0047-0740(85)90025-7.

Abstract

The whole body distribution of IAMP was studied in mice, rats, rabbits, dogs and marmosets by tissue counting, scintigraphy and quantitative macroautoradiography. Identical distribution patterns of IAMP were observed in these species showing high concentration in the brain, lungs, eyes, liver and kidneys. Following the initial distribution, IAMP was released from the lungs and accumulated in the blood and liver. In the cerebrum the activity decreased with time whereas it progressively increased in the eyes and juxtamedullary region of kidneys. The effect of ACTH, propranolol and metopyrone (metyrapone, USP) on the distribution of IAMP was studied in normal mice. The distribution of IAMP in Dahl salt-sensitive hypertensive rats was compared to Dahl salt-sensitive normotensive rats. Blocking doses of potassium iodide (KI) in marmosets and rats did not affect the distribution pattern of IAMP. Carrier amphetamine in doses of up to 1.5 mg/kg also did not significantly alter the biodistribution of IAMP. When higher doses (up to 8.0 mg/kg) were given, the activity in the gut, lungs, and liver decreased but there was no effect on the uptake in the brain, kidneys, eyes, adrenals, muscle and spleen. This suggests a higher ratio of saturable to nonsaturable binding sites in the latter organs.

摘要

通过组织计数、闪烁扫描和定量宏观放射自显影法,研究了IAMP在小鼠、大鼠、兔子、狗和狨猴体内的全身分布情况。在这些物种中观察到IAMP具有相同的分布模式,在脑、肺、眼、肝和肾中浓度较高。在初始分布之后,IAMP从肺中释放出来并在血液和肝脏中蓄积。在大脑中,活性随时间降低,而在眼和肾的近髓区域中则逐渐增加。在正常小鼠中研究了促肾上腺皮质激素、普萘洛尔和甲吡酮(美替拉酮,美国药典)对IAMP分布的影响。将IAMP在Dahl盐敏感型高血压大鼠中的分布与Dahl盐敏感型正常血压大鼠进行了比较。在狨猴和大鼠中使用阻断剂量的碘化钾(KI)并不影响IAMP的分布模式。剂量高达1.5mg/kg的载体苯丙胺也未显著改变IAMP的生物分布。当给予更高剂量(高达8.0mg/kg)时,肠道、肺和肝脏中的活性降低,但对脑、肾、眼、肾上腺、肌肉和脾脏的摄取没有影响。这表明后一组器官中可饱和结合位点与不可饱和结合位点的比例更高。

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