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Tottmar O, Hellstrom E, Holmberg K, Lindros KO: Effects of dopamine-beta-hydroxylase inhibitors FLA-57 and FLA-63 on ethanol metabolism and aldehyde dehydrogenase activity in rats. Acta Pharmacol Toxicol. 1982 Sep;51(3):198-202.
In rats pretreated with the dopamine-beta-hydroxylase (DBH)-inhibitors FLA-57 and FLA-63 (60 mg/kg, intraperitoneally, for 4 and 18 hrs), no effects on the blood acetaldehyde level after ethanol administration or on the activity of the low-Km aldehyde dehydrogenase (ALDH) in the liver were found. FLA-63 but not FLA-57 decreased the rate of ethanol elimination. FLA-63 inhibited the low-Km enzyme in vitro, but much less than the ALDH-inhibitors disulfiram and cyanamide. FLA-57 caused no inhibition in vitro. The results show that the previously observed suppression of ethanol intake in rats by FLA-57 and FLA-63 was not caused by an acetaldehyde-mediated aversion such as during the disulfiram-ethanol reaction. |
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