S-甲基-N,N-二乙基硫代氨基甲酸盐砜，一种大鼠肝脏线粒体低Km醛脱氢酶的体外和体内抑制剂。
S-methyl N,N-diethylthiolcarbamate sulfone, an in vitro and in vivo inhibitor of rat liver mitochondrial low Km aldehyde dehydrogenase.
作者信息
Nagendra S N, Madan A, Faiman M D
机构信息
Department of Pharmacology and Toxicology, University of Kansas Lawrence 60045.
出版信息
Biochem Pharmacol. 1994 Apr 20;47(8):1465-7. doi: 10.1016/0006-2952(94)90350-6.
S-Methyl N,N-diethylthiolcarbamate sulfone (DETC-Me sulfone) was investigated for its rat liver mitochondrial low Km aldehyde dehydrogenase (ALDH2) inhibitory properties. DETC-Me sulfone inhibited ALDH2 in vitro (IC50 = 3.8 microM) and in vivo (ID50 = 170 mumol/kg; 31 mg/kg). Maximum inhibition (60%) of ALDH2 was observed 8 hr after DETC-Me sulfone administration. In addition, incubation of S-methyl N,N-diethylthiolcarbamate (DETC-Me) or S-methyl N,N-diethylthiolcarbamate sulfoxide (DETC-Me sulfoxide) with rat liver microsomes and an NADPH-generating system failed to produce DETC-Me sulfone. Furthermore, DETC-Me sulfone could not be detected in plasma from rats treated with either DETC-Me sulfoxide or DETC-Me sulfone. In conclusion, DETC-Me sulfone inhibited ALDH2 in vitro and in vivo. However, there was no evidence suggesting that DETC-Me sulfoxide was metabolized to DETC-Me sulfone.
对S-甲基-N,N-二乙基硫代氨基甲酸盐砜（DETC-Me砜）的大鼠肝脏线粒体低Km醛脱氢酶（ALDH2）抑制特性进行了研究。DETC-Me砜在体外（IC50 = 3.8 microM）和体内（ID50 = 170 mumol/kg；31 mg/kg）均能抑制ALDH2。在给予DETC-Me砜后8小时观察到ALDH2的最大抑制率（60%）。此外，S-甲基-N,N-二乙基硫代氨基甲酸盐（DETC-Me）或S-甲基-N,N-二乙基硫代氨基甲酸盐亚砜（DETC-Me亚砜）与大鼠肝脏微粒体及一个产生NADPH的系统一起孵育时，未能生成DETC-Me砜。而且，在用DETC-Me亚砜或DETC-Me砜处理的大鼠血浆中未检测到DETC-Me砜。总之，DETC-Me砜在体外和体内均能抑制ALDH2。然而，没有证据表明DETC-Me亚砜会代谢为DETC-Me砜。
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