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一种新的甘草次酸衍生物的心血管作用。

Cardiovascular action of a new carbenoxolone derivative.

作者信息

Filczewski M, Kosmala M, Oledzka K

机构信息

Institute of Pharmaceutical Industry, Department of Pharmacology, Warszawa, Poland.

出版信息

Pol J Pharmacol Pharm. 1988 May-Jun;40(3):233-9.

PMID:3241764
Abstract

The circulatory effects of oleanoic acid sodium hydrogen succinate (OSS), an analogue of the anti-ulcer drug, carbenoxolone, were investigated. As carbenoxolone produces such adverse effects as sodium retention and a subsequent elevation of the arterial blood pressure in man, the present study was aimed at determining whether OSS is similar or different from it in this respect. Carbenoxolone, (43,3 mg/kg po) and OSS (66,6 mg/kg po) were given to rats twice daily for 4 weeks. The systolic blood pressure was elevated already after the first week of treatment. The hypertension was accompanied by bradycardia, which increased with the time of treatment. In the blood an increase in the creatinine level, a decrease in the urea level, and a slight elevation in sodium concentration were found after the treatment, while the potassium concentration during the whole treatment period (4 weeks) remained unchanged. Although the principal aldosterone-like effects of carbenoxolone were attributed to the oxygen presence in position 11 of the glycyrrhetinic acid ring, [8], the absence of an oxygen at that position in OSS did not cause the loss of the adverse circulatory effect.

摘要

研究了抗溃疡药物甘珀酸的类似物琥珀酸氢齐墩果酸(OSS)的循环系统作用。由于甘珀酸会产生诸如钠潴留以及随后人体动脉血压升高等不良反应,本研究旨在确定OSS在这方面与甘珀酸是相似还是不同。给大鼠每日两次口服甘珀酸(43.3毫克/千克)和OSS(66.6毫克/千克),持续4周。治疗第一周后收缩压就已升高。高血压伴有心动过缓,且心动过缓随治疗时间延长而加重。治疗后血液中肌酐水平升高、尿素水平降低、钠浓度略有升高,而整个治疗期间(4周)钾浓度保持不变。尽管甘珀酸的主要醛固酮样作用归因于甘草次酸环11位上的氧的存在,[8],但OSS在该位置没有氧并不会导致不良循环作用的丧失。

相似文献

1
Cardiovascular action of a new carbenoxolone derivative.一种新的甘草次酸衍生物的心血管作用。
Pol J Pharmacol Pharm. 1988 May-Jun;40(3):233-9.
2
Gastric and systemic effects of carbenoxolone and its derivative ISF 2715 in humans.甘珀酸及其衍生物ISF 2715对人体的胃部和全身影响。
Adv Prostaglandin Thromboxane Leukot Res. 1987;17A:361-5.
3
[Behavior of gastrin, renin, aldosterone and electrolytes after administration of deglycyrrhizinized liquorice and carbenoxolone in healthy subjects].[健康受试者服用去甘草酸甘草甜素和生胃酮后胃泌素、肾素、醛固酮及电解质的变化]
Z Gastroenterol. 1976 Apr;14(2):273-6.
4
The effects of sodium carbenoxolone on the stability of cellular membranes.甘草次酸钠对细胞膜稳定性的影响。
Scand J Gastroenterol Suppl. 1980;65:3-10.
5
The influence of amiloride on the therapeutic and metabolic effects of carbenoxolone in patients with gastric ulcer. A double-blind controlled trial.氨氯吡咪对患有胃溃疡的患者中甘珀酸的治疗及代谢作用的影响。一项双盲对照试验。
Scand J Gastroenterol Suppl. 1980;65:51-7.
6
Serum carbenoxolone: ulcer-healing and metabolic effects.血清甘草次酸:溃疡愈合及代谢效应。
Scand J Gastroenterol Suppl. 1980;65:41-8.
7
Final report on the safety assessment of Glycyrrhetinic Acid, Potassium Glycyrrhetinate, Disodium Succinoyl Glycyrrhetinate, Glyceryl Glycyrrhetinate, Glycyrrhetinyl Stearate, Stearyl Glycyrrhetinate, Glycyrrhizic Acid, Ammonium Glycyrrhizate, Dipotassium Glycyrrhizate, Disodium Glycyrrhizate, Trisodium Glycyrrhizate, Methyl Glycyrrhizate, and Potassium Glycyrrhizinate.关于甘草次酸、甘草次酸钾、琥珀酰甘草次酸二钠、甘草次酸甘油酯、甘草次酸硬脂酰酯、硬脂酰甘草次酸酯、甘草酸、甘草酸铵、甘草酸钾、甘草酸钠、甘草酸三钠、甘草酸甲酯和甘草酸锌安全性评估的最终报告。
Int J Toxicol. 2007;26 Suppl 2:79-112. doi: 10.1080/10915810701351228.
8
Carbenoxolone patients with gastric ulcers. A double-blind trial.甘珀酸治疗胃溃疡患者。一项双盲试验。
Scand J Gastroenterol Suppl. 1980;65:59-62.
9
The mechanism of mineralocorticoid action of carbenoxolone.甘草次酸的盐皮质激素作用机制。
Endocrinology. 1982 Nov;111(5):1683-6. doi: 10.1210/endo-111-5-1683.
10
The effects of piretanide capsules on blood pressure during ergometric and isometric work loads in patients with mild to moderate essential hypertension.吡咯他尼胶囊对轻至中度原发性高血压患者在测力和等长运动负荷期间血压的影响。
Pharmatherapeutica. 1985;4(6):356-66.