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胃紧张素的药理作用。

Pharmacological actions of pepsitensin.

作者信息

BLAIR A M

出版信息

Br J Pharmacol Chemother. 1962 Apr;18(2):255-74. doi: 10.1111/j.1476-5381.1962.tb01406.x.

Abstract

In confirmation of the results of Croxatto and his co-workers, plasma proteins incubated with pepsin yielded a substance (pepsitensin) with pressor activity. Euglobulin gave a much higher yield than the other plasma protein fractions. Incubation for 4 hr at pH 4 gave high yields of pressor activity (pepsitensin) but no antidiuretic activity; incubation of euglobulin for 4 hr at pH 2.5 yielded extracts with antidiuretic as well as pressor activity. Incubation for 8 to 11 hr at pH 2.5 produced the highest yield of both activities. Further incubation, at the same pH, up to 20 hr caused a rapid decline in the pressor activity of the extracts, but the antidiuretic activity was much more resistant to destruction by pepsin. Pepsitensin was found to be very soluble in water and poorly soluble in organic solvents. It is not inactivated by thioglycollate. In blood pressure assays some animals did not respond to pepsitensin, and nephrectomized (17 to 24 hr) rats were found to be more suitable preparations. Pepsitensin was shown to exert pressor effect by direct action on the blood vessels. Its pressor action could be differentiated from that of tyramine, dimethylphenylpiperazine, nicotine, noradrenaline and Pitressin but not from that of angiotensin. The isolated guinea-pig ileum and the rat uterus were equally sensitive to angiotensin and pepsitensin. In paper chromatograms, in the solvent system butanol-acetic acid-water, the R(F) of pepsitensin was very similar to that of angiotensin.

摘要

为证实克罗克萨托及其同事的研究结果,用胃蛋白酶孵育血浆蛋白可产生一种具有升压活性的物质(胃蛋白酶血管紧张素)。优球蛋白产生的量比其他血浆蛋白组分高得多。在pH 4下孵育4小时可产生高产量的升压活性物质(胃蛋白酶血管紧张素),但无抗利尿活性;在pH 2.5下将优球蛋白孵育4小时,得到的提取物同时具有抗利尿和升压活性。在pH 2.5下孵育8至11小时,两种活性的产量最高。在相同pH下进一步孵育长达20小时,提取物的升压活性迅速下降,但抗利尿活性对胃蛋白酶的破坏更具抵抗力。发现胃蛋白酶血管紧张素极易溶于水,难溶于有机溶剂。它不会被巯基乙酸盐灭活。在血压测定中,一些动物对胃蛋白酶血管紧张素无反应,发现肾切除(17至24小时)的大鼠是更合适的实验对象。胃蛋白酶血管紧张素通过直接作用于血管发挥升压作用。它的升压作用可与酪胺、二甲基苯基哌嗪、尼古丁、去甲肾上腺素和加压素的升压作用区分开来,但与血管紧张素的升压作用无法区分。分离的豚鼠回肠和大鼠子宫对血管紧张素和胃蛋白酶血管紧张素同样敏感。在纸色谱中,在正丁醇 - 乙酸 - 水溶剂系统中,胃蛋白酶血管紧张素的R(F)与血管紧张素的R(F)非常相似。

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