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首页> 外文期刊>Canadian Journal of Physiology and Pharmacology >The biochemical and pharmacological properties of a newly synthesized H+-K+ ATPase inhibitor, 2-dimethylamino-4,5-dihydrothiazolo(4,5:3,4)pyridol-(1,2-a)benzimidazol e.
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The biochemical and pharmacological properties of a newly synthesized H+-K+ ATPase inhibitor, 2-dimethylamino-4,5-dihydrothiazolo(4,5:3,4)pyridol-(1,2-a)benzimidazol e.

机译：新合成的H + -K + ATPase抑制剂2-二甲基氨基-4,5-二氢噻唑并（4,5：3,4）吡啶-（1,2-a）苯并咪唑e的生化和药理特性。

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摘要

This study was designed to determine the effect of a newly synthesized proton pump inhibitor, 2-dimethylamino-4,5-dihydrothiazolo[4,5:3,4]pyridol[1,2-a]be nzimidazole (YJA20379-2), on gastric H(+)-K(+) ATPase activity, acid secretion, and experimental gastroduodenal lesions or ulcers in rats. YJA20379-2 inhibited in a concentration-dependent manner the proton pump (H(+)-K(+) ATPase) activity in isolated hog gastric mucosal microsomes, therefore, confirming its classification as a proton pump inhibitor. The inhibitory efficacy of YJA20379-2 on the proton pump was about eight times higher than that of omeprazole at pH 7.4. The activity of the inhibited enzyme was not restored by dilution and washout method, so this implied that the inhibition of YJA20379-2 is not reversible. YJA20379-2, given intraduodenally or orally, potently suppressed acid secretion in pylorus-ligated rats, with ED50 values of 3.6 and 7.7 mg.kg(-1), respectively. Pretreatment with YJA20379-2 dose dependently protected the gastric mucosa from damage induced by absolute ethanol, water-immersion stress, indomethacin, and the duodenal mucosa from damage induced by mepirizole in rats, with ED50 values of 11.0, 21.0, 0.5, and 18.7 mg.kg(-1), respectively. Repeated administration of YJA20379-2 also dose dependently accelerated spontaneous healing of acetic acid induced gastric ulcers. These results suggest that YJA20379-2 has potent antisecretory and antiulcer effects, which are exerted by suppression of H(+)-K(+) ATPase activity in gastric parietal cells, such that YJA20379-2 may be useful for the clinical treatment of peptic ulcer diseases.
机译：这项研究旨在确定新合成的质子泵抑制剂2-二甲基氨基-4,5-二氢噻唑[4,5：3,4]吡啶[1,2-a] be咪唑（YJA20379-2）的作用，对大鼠胃H（+）-K（+）ATPase活性，酸分泌和实验性胃十二指肠病变或溃疡的影​​响。 YJA20379-2以浓度依赖性的方式抑制分离的猪胃黏膜微粒体中的质子泵（H（+）-K（+）ATPase）活性，因此确认其为质子泵抑制剂的分类。在pH 7.4时，YJA20379-2对质子泵的抑制作用是奥美拉唑的约八倍。通过稀释和洗脱方法不能恢复抑制酶的活性，因此这表明对YJA20379-2的抑制是不可逆的。 YJA20379-2经十二指肠内或口服给予可有效抑制幽门结扎大鼠的酸分泌，ED50分别为3.6和7.7 mg.kg（-1）。 YJA20379-2预处理可剂量依赖性地保护胃粘膜免受无水乙醇，水浸应力，吲哚美辛和十二指肠粘膜的损害，不受美吡唑的损害，ED50值为11.0、21.0、0.5和18.7 mg .kg（-1）。重复给药YJA20379-2还可以剂量依赖性地加速乙酸诱导的胃溃疡的自发愈合。这些结果表明，YJA20379-2具有有效的抗分泌和抗溃疡作用，其作用是通过抑制胃壁细胞中的H（+）-K（+）ATPase活性来实现的，因此YJA20379-2可能对临床消化道疾病有用。溃疡病。

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