Nitrobenzylthioinosine binding in brain: an interspecies study.
Nitrobenzylthioinosine binding in brain: an interspecies study.
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硝基苄基硫代肌苷在大脑中的结合：一项种间研究。
DOI：
10.1016/0024-3205(85)90071-2
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发表时间：
1985
期刊：
影响因子：
6.1
通讯作者：
P. Marangos
中科院分区：
文献类型：
--
作者：
A. Verma;P. Marangos
研究了强效腺苷摄取抑制剂[3H]硝基苄基硫代肌苷（[3H]NBI）与人、狗、豚鼠、大鼠和小鼠脑皮质膜制剂的结合。在这五种植物中均发现了具有相似动力学参数的可逆、特异、饱和、高亲和力的结合。（Kd=0.16-0.44nM; Bmax=128-196 fmol/mg prot）。地拉西普、己苯定和双嘧达莫在人、狗、豚鼠和小鼠制剂中均是[3H]NBI结合的高效抑制剂，而在大鼠中没有。这些化合物显示出对[3H]NBI结合的竞争性抑制，表明它们在同一位点起作用。在大鼠身上看到的差异似乎是一种独特的、与物种相关的异常现象。二氢吡啶钙拮抗剂也抑制结合，但其效力低于腺苷摄取阻滞剂。这种抑制在狗和人身上最有效，这表明钙通道和腺苷摄取位点之间存在关系。
The binding of the potent adenosine uptake inhibitor [3H]nitrobenzylthioinosine ([3H]NBI) to cerebral cortical membrane preparations from human, dog, guinea pig, rat, and mouse was investigated. Reversible, specific, saturable, high affinity binding was found in all five species with similar kinetic parameters. (Kd=0.16-0.44nM; Bmax=128-196 fmol/mg prot.). Dilazep, hexobendine, and dipyridamole were all high potency inhibitors of [3H]NBI binding in human, dog, guinea pig and mouse preparations but not in rat. These compounds showed a competitive inhibition of [3H]NBI binding indicating that they are acting at the same site. Discrepancies seen in the rat appear to be a unique, species related anomaly. The dihydropyridine calcium antagonists also inhibited binding with lower potency than the adenosine uptake blockers. This inhibition was most potent in dog and human and suggests a relationship between the calcium channel and the adenosine uptake site.
哺乳动物细胞中核苷转运的异质性。
影响因子：
3.6
作者：
Belt,JA
通讯作者：
Belt,JA