LIVER ALCOHOL AND ALDEHYDE DEHYDROGENASE - INHIBITION AND POTENTIATION BY HISTAMINE AGONISTS AND ANTAGONISTS

被引：62

作者：

MESSIHA, FS

HUGHES, MJ

机构：

[1] TEXAS TECH UNIV,SCH MED,DEPT PATHOL,PSYCHOPHARMACOL LAB,LUBBOCK,TX 79409

[2] TEXAS TECH UNIV,SCH MED,DEPT PSYCHIAT,PSYCHOPHARMACOL LAB,LUBBOCK,TX 79409

[3] TEXAS TECH UNIV,SCH MED,DEPT PHYSIOL,LUBBOCK,TX 79409

来源：

CLINICAL AND EXPERIMENTAL PHARMACOLOGY AND PHYSIOLOGY | 1979年 / 6卷 / 03期

关键词：

betazole; burimamide; diphenhydramine; H[!sub]1[!/sub]‐ and H[!sub]2[!/sub]‐receptor antagonists; H[!sub]1[!/sub]‐and H[!sub]2[!/sub]‐receptor agonists; histamine; liver alcohol dehydrogenase; liver aldehyde dehydrogenase metiamide; toxic effect of ethanol;

D O I：

10.1111/j.1440-1681.1979.tb01250.x

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

1. The in vitro effects of histamine, some other Hi‐ and H2‐receptor agonists and some antagonists were studied on the specific activities and kinetics of rat liver alcohol dehydrogenase (ADH), and cytoplasmic and mitochondrial liver aldehyde dehydrogenase (ALDH). 2. Histamine (H1‐ and H2‐agonist) non‐competitively inhibited ADH and ALDH, 2‐(2‐aminoethyl) pyridine (Hi‐receptor agonist) non‐competitively inhibited ADH. There were no changes of cytoplasmic and mitochondrial liver ALDH activities in the presence of 2‐(2‐aminoethyl) pyridine. 3. Betazole (H2‐receptor agonist) produced a competitive inhibition of mitochondrial ALDH but not of ADH or cytoplasmic ALDH. 4. Diphenhydramine (H1‐receptor antagonist) non‐competitively inhibited ADH at a lower concentration. It stimulated mitochondrial ALDH activity without changes in cytoplasmic ALDH from control values. 5. Burimamide (H2‐receptor antagonist) produced a biphasic and dose‐dependent stimulation and non‐competitive inhibition of ADH and it non‐competitively inhibited ALDH in both cytoplasmic and mitochondrial fractions. Metiamide (H2‐receptor antagonist) non‐competitively inhibited all ADH and ALDH of both liver fraction studied. 6. It is concluded that liver ADH and ALDH activity can be altered by compounds which affect both Hi‐ and H2‐histamine receptors and that these compounds may cause an in vivo potentiation and/or reduction of the toxic effect of ethanol. Copyright © 1979, Wiley Blackwell. All rights reserved

引用

页码：281 / 292

页数：12

共 27 条

[1] STUDIES ON MODE OF ACTION OF HISTAMINE H1 RECEPTOR ANTAGONISTS AND H2-RECEPTOR ANTAGONISTS ON GASTRIC HISTAMINE METHYLTRANSFERASE [J].