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丙磺舒对肾皮质切片中氨基酸积累影响的研究。

A study of the probenecid effect on amino acid accumulation in kidney cortex slices.

作者信息

Wack A, Woermann C, Braun W

出版信息

Arch Int Pharmacodyn Ther. 1982 Apr;256(2):292-300.

PMID:7103616
Abstract

The amount of amino acids accumulated by rat and mouse kidney cortex slices is determined by both membrane transport and intracellular metabolism, especially protein incorporation. Even with substrate concentrations of 100 microM up to 70% of the transported amino acids were found to be protein incorporated. Probenecid reduces the accumulation of the amino acids glycine, L-phenylalanine, L-valine, L-arginine, L-lysine, L-proline and alpha-AIB. At substrate concentrations of 100 microM the inhibition is between 28 and 66% (except alpha-AIB) with a probenecid concentration of 7.0 mM. Slight inhibitory effects were observed with 0.7 mM probenecid. The probenecid effect, however, is mainly on the protein incorporation. With 7.0 mM probenecid protein incorporation is reduced considerably, for some amino acids below 10% of the control values; small inhibitory effects were observed with concentrations of 0.7 mM. Amino acid transport is affected only slightly by probenecid. In consequence, higher accumulation rates of free amino acids may be measured after probenecid administration, preferentially with amino acids showing high initial incorporation rates.

摘要

大鼠和小鼠肾皮质切片积累的氨基酸量由膜转运和细胞内代谢共同决定,尤其是蛋白质掺入过程。即使底物浓度达到100微摩尔/升,仍发现高达70%的转运氨基酸被掺入蛋白质中。丙磺舒可减少甘氨酸、L-苯丙氨酸、L-缬氨酸、L-精氨酸、L-赖氨酸、L-脯氨酸和α-氨基异丁酸等氨基酸的积累。在底物浓度为100微摩尔/升时,丙磺舒浓度为7.0毫摩尔时,抑制率在28%至66%之间(α-氨基异丁酸除外)。丙磺舒浓度为0.7毫摩尔时观察到轻微抑制作用。然而,丙磺舒的作用主要在于蛋白质掺入。丙磺舒浓度为7.0毫摩尔时,蛋白质掺入量大幅减少,某些氨基酸的掺入量低于对照值的10%;丙磺舒浓度为0.7毫摩尔时观察到轻微抑制作用。丙磺舒对氨基酸转运的影响较小。因此,给予丙磺舒后可测得游离氨基酸的积累率更高,尤其是对于初始掺入率较高的氨基酸。

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