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肾上腺素能阻滞剂和兴奋剂及抗甲状腺药对鼠肝T4-5′-脱碘酶活性的影响

ADRENERGIC ANTAGONIST AND AGONIST AND ANTITHYROID DRUGS ON THE ACTIVITY OF HEPATIC T4-5’-DEIODINASE IN RATS

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【摘要】 采用体外实验研究外周T4转变为T3的脱单碘作用和能调节此过程的药物。T4转变为T3时,T4的km值为7.77μM,Vmax为每分钟1.33pmol/mg蛋白质。心得安、心得舒、美多心安、肾上腺素、去甲肾上腺素、异丙肾上腺素、育红宾、丙基硫氧嘧啶和甲基硫氧嘧啶均能抑制该酶活性,且与剂量有关,而cAMP、他巴唑无抑制作用。

【Abstract】 An in vitro model was used to study peripheral monodeiodination of thryoxine to triiodothyronine(T3)and the grugs capable of modulating it.The enzyme gave a Km of 7.77 μm for T4,and a Vmax of 1.33 pmol/min per mgofprotein.Propranolol,alprenolol,metopralol,epinephrine,norepinephrine,isoproterenol and yohimbine,propylthiouracil and methylthiouracil inhibited the enzyme in a dosedependent manner,cAMP and methimazole did not inhibit the enzyme.

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