Zakusov V V, Mineeva-Vialykh M F
Biull Eksp Biol Med. 1976 Sep;82(9):1071-3.
The influence of cocaine on tyrosine hydroxilase of rat brain hypothalamus was investigated in vivo (0.5 mg/kg) and in vitro (10(--6)--10(--5)M). Cocaine was used as a substance with a known adrenergic type of action. It was shown that under standard conditions cocaine in vitro increased the enzyme activity and decreased the Km for DMPH4 cofactor without changing Vmax of the reaction analyzed by the membrane enzyme. Cocaine in vitro decreased the tyrosine hydroxylase activity, especially that of the membrane enzyme. In this case there occurred a decrease of Km for DMPH4 and a decrease of Vmax of the reaction. The decrease of Vmax is considered to be the result of the secondary effect of cocaine.
研究了可卡因在体内(0.5毫克/千克)和体外(10(-6)-10(-5)摩尔)对大鼠脑下丘脑酪氨酸羟化酶的影响。可卡因被用作一种具有已知肾上腺素能作用类型的物质。结果表明,在标准条件下,体外可卡因增加了酶活性,降低了DMPH4辅因子的米氏常数(Km),而不改变膜酶分析反应的最大反应速度(Vmax)。体外可卡因降低了酪氨酸羟化酶活性,尤其是膜酶的活性。在这种情况下,DMPH4的Km降低,反应的Vmax降低。Vmax的降低被认为是可卡因继发效应的结果。