disulfiram

Disulfiram (TETD) 是一种乙醛脱氢酶 ALDH 的抑制剂，抑制 hALDH1 和 hALDH2 (IC50=0.15 1.45 μM)，具有特异性。Disulfiram 对酒精产生急性敏感性，还可以抑制 GSDMD 孔形成。

2-(1H-Indol-3-yl)ethan-1-ol (3-(2-Hydroxyethyl)indole) 是在双硫仑治疗后在肝脏中形成的代谢物，可诱导人类睡眠。它也是酒精发酵的二次产物。

EWP 815是一种二硫仑类似物，是 Ins(1,4) P 2磷酸酶、Ins(1,4,5) P 3 5-磷酸酶和多巴胺β-羟化酶活性的强效抑制剂[1] [2]。

Methyl diethyldithiocarbamate is an active metabolite of the aldehyde dehydrogenase inhibitor disulfiram .1It is produced by methylation of the disulfiram metabolite diethyldithiocarbamate in mouse liver microsomes.2Methyl diethyldithiocarbamate inhibits liver low Kmaldehyde dehydrogenase (ALDH) in rats (ID50= 15.5 mg/kg).1It decreases mean arterial pressure (MAP) and increases heart rate during ethanol challenge in rats when administered at a dose of 20.6 mg/kg. 1.Hart, B.W., Yourick, J.J., and Faiman, M.D.S-methyl-N,N-diethylthiolcarbamate: A disulfiram metabolite and potent rat liver mitochondrial low Km aldehyde dehydrogenase inhibitorAlcohol7(2)165-169(1990) 2.Gessner, T., and Jakubowski, M.Diethyldithiocarbamic acid methyl ester. A metabolite of disulfiramBiochem. Pharmacol.21(2)219-230(1972)

MeDTC (S-Methyl-N,N-diethylthiocarbamate Sulfone), 作为 Disulfiram 的一种代谢产物，它是一种高效的不可逆 ALDH (醛脱氢酶) 抑制剂。