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2,6 - 二甲基吡啶 - N - 氧化物的抗缺氧活性

ANTIHYPOXIC ACTIVITY OF 2,6-DIMETHYLPYRIDINE-N-OXIDE.

作者信息

Vasetska Olesia P, Prodanchuk Mykola G, Zhminko Petro G

机构信息

L.I. MEDVED'S RESEARCH CENTER OF PREVENTIVE TOXICOLOGY, FOOD AND CHEMICAL SAFETY, MINISTRY OF HEALTH OF UKRAINE (STATE ENTERPRISE), KYIV, UKRAINE.

出版信息

Wiad Lek. 2022;75(12):2974-2981. doi: 10.36740/WLek202212114.

Abstract

OBJECTIVE

The aim: To study the antihypoxic activity of 2,6-dimethylpyridine-N-oxide in mice using the various experimental models of acute hypoxia under orally or intraperitoneally administration.

PATIENTS AND METHODS

Materials and methods: The studies were performed on male CD-1 (SPF) mice. The antihypoxic activity of 2,6-dimethylpyridine-N-oxide was studied in three experimental models of acute hypoxia - hypercapnic hypoxia or hypoxia in a closed space, hemic hypoxia and histotoxic hypoxia at orally administration at doses 0.07; 7.1 and 71 mg/kg (respectively 1/20000, 1/200 and 1/20 of LD50) and at intraperitoneally administration at doses 7.1 and 71 mg/kg in comparison with reference drug Armadin.

RESULTS

Results: It is established, that 2,6-dimethylpyridine-N-oxide shows a antihypoxic activity in the all experimental models of acute hypoxia (hypoxia in a closed space, hemic hypoxia and histotoxic hypoxia). Its antihypoxic activity in acute hemic hypoxia and in acute hypoxia in a closed space was significantly higher than of reference drug Armadin, but during acute histotoxic hypoxia did not differ from Armadin. Also at intraperitoneal administration of 2,6-dimethylpyridine-N-oxide demonstrates less pronounced antihypoxic activity than at oral administration in all experimental models of acute hypoxia, but the coefficient efficiency is higher than in the reference drug Armadin.

CONCLUSION

Conclusions: 2,6-dimethylpyridine-N-oxide may be recommended for further detailed experimental studies as a perspective antihypoxant.

摘要

目的

研究2,6-二甲基吡啶-N-氧化物在小鼠急性缺氧的各种实验模型中经口服或腹腔注射给药后的抗缺氧活性。

患者和方法

材料与方法:研究选用雄性CD-1(无特定病原体)小鼠。在三种急性缺氧实验模型中研究2,6-二甲基吡啶-N-氧化物的抗缺氧活性,即高碳酸血症性缺氧或密闭空间缺氧、血液性缺氧和组织中毒性缺氧,口服剂量分别为0.07、7.1和71mg/kg(分别为半数致死量的1/20000、1/200和1/20),腹腔注射剂量为7.1和71mg/kg,并与参比药物阿尔马丁作比较。

结果

结果表明,2,6-二甲基吡啶-N-氧化物在所有急性缺氧实验模型(密闭空间缺氧、血液性缺氧和组织中毒性缺氧)中均表现出抗缺氧活性。其在急性血液性缺氧和急性密闭空间缺氧中的抗缺氧活性显著高于参比药物阿尔马丁,但在急性组织中毒性缺氧中与阿尔马丁无差异。此外,在所有急性缺氧实验模型中,腹腔注射2,6-二甲基吡啶-N-氧化物的抗缺氧活性均不如口服明显,但其效价比高于参比药物阿尔马丁。

结论

结论:2,6-二甲基吡啶-N-氧化物作为一种有前景的抗缺氧剂,可推荐用于进一步详细的实验研究。

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