The hypolipidemic activity of N(4-methyl-phenyl)diphenimide in rodents.
N(4-Methyl-phenyl)diphenimide afforded potent hypolipidemic activity in rodents. Serum cholesterol levels were reduced 67% and serum triglyceride were lowered 66% in rats by the drug after two weeks administration orally at 20 mg/kg/day. Rate limiting enzymes in the de novo synthesis of lipids in the liver were suppressed by the drug. Cholesterol was also removed from the body due to the drug accelerating bile excretion. Lipids removed from the blood compartment were not deposited in the organs of the body. VLDL and LDL cholesterol content was significantly reduced in rats treated with the drug with marked increase in HDL cholesterol after two weeks of administration. These data suggest that the drug may be useful in hyperlipidemic states and atherosclerosis in man, thus, further investigation of this class of chemicals is warranted.
Hall
I H
IH
Division of Medicinal Chemistry and Natural Products, School of Pharmacy, University of North Carolina, Chapel Hill 27514.
Wong
O T
OT
Murthy
A R
AR
Day
P A
PA
Calvin
J
J
D000818:Animals; D001646:Bile / Q000378:metabolism; D002784:Cholesterol / Q000378:metabolism; D003984:Dibenzazepines / Q000494:pharmacology* / Q000633:toxicity; D005243:Feces / Q000032:analysis; D000960:Hypolipidemic Agents / Q000633:toxicity; D066298:In Vitro Techniques; D007421:Intestine, Small / Q000187:drug effects / Q000378:metabolism; D050356:Lipid Metabolism; D008074:Lipoproteins / Q000097:blood; D008099:Liver / Q000187:drug effects / Q000201:enzymology / Q000378:metabolism; D008297:Male; D051379:Mice; D051381:Rats; D011919:Rats, Inbred Strains; D014280:Triglycerides / Q000378:metabolism
D003984:Dibenzazepines; D000960:Hypolipidemic Agents; D008074:Lipoproteins; D014280:Triglycerides; C055530:N-(4-methylphenyl)diphenimide; D002784:Cholesterol