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泛硫乙胺,一种半胱胺前体,可使大鼠体内的免疫反应性生长抑素和催乳素减少。

Pantethine, a cysteamine precursor, depletes immunoreactive somatostatin and prolactin in the rat.

作者信息

Reichlin S, Bollinger-Gruber J A

出版信息

Endocrinology. 1985 Aug;117(2):492-5. doi: 10.1210/endo-117-2-492.

Abstract

Pantethine, a stable disulfide precursor of pantetheine, has been reported to increase intracellular concentration of cysteamine in cultured fibroblasts of patients with cystinosis. In order to determine whether pantethine acts like cysteamine in bringing about depletion of immunoreactive somatostatin (IRS) in rat neural and gastrointestinal tissues and depletion of immunoreactive PRL (IRPRL) in the anterior pituitary, groups of male rats were given pantethine by ip injection at a dose of 0.264 mM or 0.528 mM/100 g body weight or normal saline and killed 4 h later. The interval chosen corresponds to the time of maximum effect after oral cysteamine administration. In cerebral cortex, hypothalamus, duodenal and gastric mucosa, and pancreas, IRS was uniformly depressed by 50% or more as compared with control rats, the most striking changes occurring in the hypothalamus where there was a 64% depletion at the higher dose of drug. Both dosage levels depleted IRPRL in pituitary and serum. At the higher dose, IRPRL was reduced by approximately 85% in the pituitary and 75% in the serum. These findings support the hypothesis that pantethine administration leads to an accumulation of cysteamine within cells throughout the body and that the cysteamine so formed depletes IRS and IRPRL.

摘要

泛硫乙胺是泛酰巯基乙胺的一种稳定二硫化物前体,据报道它能增加胱氨酸病患者培养成纤维细胞内半胱胺的浓度。为了确定泛硫乙胺在导致大鼠神经和胃肠道组织中免疫反应性生长抑素(IRS)耗竭以及垂体前叶中免疫反应性催乳素(IRPRL)耗竭方面是否与半胱胺作用相似,给雄性大鼠组腹腔注射剂量为0.264 mM或0.528 mM/100 g体重的泛硫乙胺或生理盐水,4小时后处死。所选择的时间间隔对应于口服半胱胺后效应最大的时间。在大脑皮层、下丘脑、十二指肠和胃黏膜以及胰腺中,与对照大鼠相比,IRS均一致降低了50%或更多,最显著的变化发生在下丘脑,在较高剂量药物作用下耗竭了64%。两个剂量水平均使垂体和血清中的IRPRL耗竭。在较高剂量时,垂体中的IRPRL降低了约85%,血清中降低了75%。这些发现支持了这样的假设,即给予泛硫乙胺会导致全身细胞内半胱胺的积累,并且如此形成的半胱胺会耗竭IRS和IRPRL。

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