（E）-2-（3,4-二甲氧基苯乙烯基）-苯甲酸甲酯（ALE-36）对H⁺，K⁺-ATP酶的抑制作用

Inhibition of H+,K+-ATPase by methyl(E)-2-(3,4-dimethoxystyryl)-benzimidazole-4-carboxylate (ALE-36).

作者信息

Yamamoto O, Tanaka H, Ueda F, Kimura K

机构信息

Research Laboratories, Nippon Shinyaku Co., Ltd., Kyoto, Japan.

出版信息

Scand J Gastroenterol Suppl. 1989;162:178-81. doi: 10.3109/00365528909091155.

DOI:10.3109/00365528909091155

PMID:2556788

Abstract

ALE-36, as well as omeprazole and SCH 28080, markedly inhibited the [14C]aminopyrine (AP) accumulation induced by dibutyryl cyclic AMP (dbcAMP) and H+,K+-ATPase activity in a concentration-dependent manner. The inhibitory effect of omeprazole on the dbcAMP-induced [14C]AP accumulation was reversed by treatment with beta-mercaptoethanol, but those of ALE-36 and SCH 28080 were not. ALE-36 and SCH 28080 did not inhibit dog renal Na+,K+-ATPase activity, while omeprazole and ouabain did inhibit this enzyme activity. These results suggest that the inhibitory action of ALE-36 on acid secretion is due to the specific inhibition of gastric H+,K+-ATPase, the manner being different from in the case of omeprazole.

摘要

ALE-36以及奥美拉唑和SCH 28080均以浓度依赖性方式显著抑制二丁酰环磷腺苷（dbcAMP）和H⁺，K⁺-ATP酶活性诱导的[¹⁴C]氨基比林（AP）蓄积。用β-巯基乙醇处理可逆转奥美拉唑对dbcAMP诱导的[¹⁴C]AP蓄积的抑制作用，但ALE-36和SCH 28080的抑制作用则不能被逆转。ALE-36和SCH 28080不抑制犬肾Na⁺，K⁺-ATP酶活性，而奥美拉唑和哇巴因则可抑制该酶活性。这些结果表明，ALE-36对胃酸分泌的抑制作用是由于对胃H⁺，K⁺-ATP酶的特异性抑制，其作用方式与奥美拉唑不同。