Ih. Hall et al., THE HYPOLIPIDEMIC EFFECTS OF 1-ACETYL-4-PHENYL-1,2,4-TRIAZOLIDINE-3,5-DIONE IN RODENTS, Pharmaceutical research, 10(8), 1993, pp. 1206-1211
1-Acetyl-4-phenyl-1,2,4-triazolidine,5-dione (APTD), a potent hypolipi
demic agent, lowered both serum cholesterol and triglyceride levels in
normo- and hyperlipidemic rats at 10 or 20 mg/kg/day. The agent effec
tively lowered VLDL-cholesterol (VLDL-C) and LDL-C content and raised
HDL-C content in normal and hyperlipidemic rats treated from 4 to 8 we
eks. Similar effects on the incorporation of cholesterol into the lipo
protein fractions were observed after drug treatment. Tissue lipids, e
.g. cholesterol, were lowered, whereas fecal cholesterol levels were i
ncreased. APTD's primary targets were acyl CoA cholesterol acyl transf
erase (ACAT) for cholesterol ester synthesis and sn-glycerol-3-phospha
te acyl transferase (GPAT) and phosphatidylate phosphohydrolase (PPH)
for triglyceride synthesis.