FLA-63诱发的多巴胺β-羟化酶抑制机制。一项体外研究。
Mechanism of inhibition of dopamine beta-hydroxylase evoked by FLA-63. An in vitro study.
作者信息
Brodde O E, Nagel M, Schümann H J
出版信息
Arch Int Pharmacodyn Ther. 1977 Aug;228(2):184-90.
Bis-(4-methyl-1-homopiperazinylthiocarbonyl)-disulphide (FLA-63) inhibits in vitro purified bovine adrenal medullary dopamine beta-hydroxylase (BDH) concentration-dependently; 50% inhibition is produced by 2 x 10(-6)M FLA-63. Spectrophotometric experiments show that FLA-63 is reduced by ascorbate very likely to the corresponding dithiocarbamate-derivative, which acts as a Cu++-chelator. Cu++-ions are able to completely abolish the inhibition of the DBH caused by FLA-63 in concentrations up to 2.5 x 10(-6)M. It is concluded that FLA-63 inhibits the DBH mainly in its reduced form via the formation of a chelate-complex with copper ions derived from the DBH.
双（4-甲基-1-高哌嗪基硫代羰基）二硫化物（FLA-63）浓度依赖性地抑制体外纯化的牛肾上腺髓质多巴胺β-羟化酶（BDH）；2×10⁻⁶M的FLA-63可产生50%的抑制作用。分光光度实验表明，抗坏血酸很可能将FLA-63还原为相应的二硫代氨基甲酸盐衍生物，该衍生物可作为铜离子螯合剂。高达2.5×10⁻⁶M浓度的铜离子能够完全消除FLA-63对DBH的抑制作用。由此得出结论，FLA-63主要以其还原形式通过与源自DBH的铜离子形成螯合物来抑制DBH。
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