Fedurina M A, Usatenko M S, Borodkin Iu S
Biull Eksp Biol Med. 1982 Sep;94(9):76-8.
The effect of IEM-611 (30 mg/kg) on alcohol consumption in rats under the conditions of voluntary choice between water and 15% ethanol was studied as that on alcohol dehydrogenase (ADH) in postmitochondrial supernatant and in NAD-dependent aldehyde dehydrogenases (A1DH) in liver mitochondria. Administration of IEM-611 during 6 or 12 days reduces ethanol consumption by 29 and 30%, respectively, activates ADH and appreciably decreases overall activity of NAD-dependent A1DH. At the same time the ADH/A1DH ratio increases. Activation of ADH and A1DH and the decreased ADH/A1DH ratio were disclosed in alcohol preferring rats as compared to water preferring animals. IEM-611 shifts enzymatic activity of ethanol metabolism towards the level characteristic for water preferring rats. It is suggested that variation of the ADH/A1DH ratio is one of the mechanisms responsible for the decreased ethanol consumption in rats.
研究了IEM - 611(30毫克/千克)在大鼠水与15%乙醇自愿选择条件下对其酒精摄入量的影响,以及对线粒体后上清液中酒精脱氢酶(ADH)和肝线粒体中NAD依赖型醛脱氢酶(A1DH)的影响。在6天或12天内给予IEM - 611分别使乙醇摄入量降低29%和30%,激活ADH并显著降低NAD依赖型A1DH的总体活性。同时,ADH/A1DH比值增加。与偏好水的动物相比,在偏好酒精的大鼠中发现ADH和A1DH被激活且ADH/A1DH比值降低。IEM - 611使乙醇代谢的酶活性朝着偏好水的大鼠的特征水平转变。提示ADH/A1DH比值的变化是导致大鼠乙醇摄入量降低的机制之一。