Carlsson A, Henning M, Lindberg P, Martinson P, Trolin G, Waldeck B, Wickberg B
Acta Pharmacol Toxicol (Copenh). 1978 Apr;42(4):292-7. doi: 10.1111/j.1600-0773.1978.tb02204.x.
Coprine or disulfiram was given to rats in various doses at various time intervals before the administration of 2 g/kg ethanol. The ratio acetaldehyde/ethanol in the alveolar air was measured by gas chromatography and was taken as an index of the aldehyde dehydrogenase (ALDH) activity. The activity of dopamine beta-hydroxylase (DBH) was estimated in the same animals by measuring the amount of 14C-octopamine formed from 14C-tyramine in the heart. Coprine and disulfiram both caused an increase in the acetylaldehyde/ethanol ratio, coprine being more potent than disulfiram. Disulfiram, but not coprine, reduced the net yield of 14C-octopamine. In rats pretreated with either coprine or disulfiram, blood-pressure and heart-rate were recorded before and after intraperitoneal injections of 0.4 g/kg ethanol. In both cases ethanol caused a marked and rapid fall in blood-pressure. However, this effect was accompanied by tachycardia only in animals treated with coprine. It is concluded that coprine like disulfiram inhibits ALDH, but only disulfiram causes an additional inhibition of DBH. This difference may account for differences in the cardiovascular response to ethanol.
在给大鼠注射2 g/kg乙醇之前，以不同剂量、在不同时间间隔给它们注射鬼伞素或双硫仑。通过气相色谱法测量肺泡气中乙醛/乙醇的比例，并将其作为醛脱氢酶（ALDH）活性的指标。通过测量心脏中由14C-酪胺生成的14C-章鱼胺的量，来估算同一批动物中多巴胺β-羟化酶（DBH）的活性。鬼伞素和双硫仑均使乙醛/乙醇比例升高，鬼伞素的作用比双硫仑更强。双硫仑降低了14C-章鱼胺的净生成量，但鬼伞素没有。在用鬼伞素或双硫仑预处理的大鼠中，在腹腔注射0.4 g/kg乙醇前后记录血压和心率。在两种情况下，乙醇均导致血压显著且迅速下降。然而，只有在用鬼伞素处理的动物中，这种效应伴随着心动过速。得出的结论是，鬼伞素与双硫仑一样抑制ALDH，但只有双硫仑会额外抑制DBH。这种差异可能解释了对乙醇心血管反应的差异。
