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大鼠肺中色甘酸钠二钠和酚红摄取与结合的比较。

Comparison of uptake and binding of disodium cromoglycate and phenol red in rat lung.

作者信息

Gardiner T H, Goodman F R

出版信息

J Pharmacol Exp Ther. 1976 Aug;198(2):395-402.

PMID:7666
Abstract

In rat lung slices 3H-disodium cromoglycate (3H-DSCG) (0.001 mM) was taken up rapidly and 3H-DSCG tissue spaces, which equilibrated by 30 minutes, remained constant over a 4-hour incubation period. In contrast, 35S-phenol red (0.001 mM) accumulated in lung slices to a much greater extent than did DSCG, and the measured tissue spaces continued to increase over a 3-hour incubation period. In the presence of either phenol red (1 mM) or the metabolic inhibitors, iodoacetic acid (10(-4) M) and dinitrophenol (10(-4) M), 3H-DSCG uptake was significantly decreased. Accumulation of 3H-DSCG in lung slices and binding to tissue homogenates (pH 7.4) was also decreased when Ca and Mg ions were omitted from the bathing solution. Although DSCG and phenol red mutually inhibited the accumulation of one another over time in lung slices and 3H-DSCG (0.001 mM) binding to lung homogenates was decreased in the presence of 1 mM phenol red, 35S-phenol red efflux was not altered by the addition of 1 mM DSCG during the washout. Thus, it appears that, in rat lung, DSCG and phenol red share a common binding site(s) for uptake, possible on the transport "carrier." Also, there appear to be additional pulmonary binding sites for phenol red. These sites are not occupied by DSCG and their presence could account for the differences observed in the extent of accumulation of the two compounds in lung slices.

摘要

在大鼠肺切片中,3H - 色甘酸钠(3H - DSCG)(0.001 mM)迅速被摄取,30分钟达到平衡的3H - DSCG组织间隙在4小时的孵育期内保持恒定。相比之下,35S - 酚红(0.001 mM)在肺切片中的积累程度比DSCG大得多,并且在3小时的孵育期内测量的组织间隙持续增加。在存在酚红(1 mM)或代谢抑制剂碘乙酸(10^(-4) M)和二硝基酚(10^(-4) M)的情况下,3H - DSCG摄取显著降低。当从浴液中省略Ca和Mg离子时,肺切片中3H - DSCG的积累以及与组织匀浆(pH 7.4)的结合也会降低。尽管DSCG和酚红在肺切片中随时间相互抑制彼此的积累,并且在存在1 mM酚红的情况下3H - DSCG(0.001 mM)与肺匀浆的结合减少,但在洗脱过程中添加1 mM DSCG不会改变35S - 酚红的流出。因此,在大鼠肺中,DSCG和酚红似乎共享一个共同的摄取结合位点,可能在转运“载体”上。此外,似乎存在酚红的额外肺结合位点。这些位点未被DSCG占据,它们的存在可以解释在肺切片中观察到的两种化合物积累程度的差异。

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