The lipid-lowering profile in rodents. AZ-1355, a new dibenzoxazepine derivative.
The lipid-lowering profile of ethyl 10,11-dihydro-4-methoxydibenz[b,f]-(1,4)oxazepine-8-carboxylate (AZ-1355) has been evaluated using clofibrate as a reference compound. This compound is structurally unrelated to any other hypolipidemic agent. AZ-1355 was selected not only for its effect in reducing serum lipids, but also because it inhibits platelet aggregation in vivo and elevates the prostaglandin I2/thromboxane A2 ratio in vitro. It lowers serum total cholesterol in Triton-treated hyperlipidemic mice, and also lowers serum total cholesterol and triglyceride in dietary hyperlipidemic rats. In golden hamsters chosen for further evaluation, AZ-1355 reduced serum, liver and cardiac lipids, improved the beta/alpha-lipoprotein ratio and increased the HDL cholesterol. Thus, it is apparent that the lipid-lowering profile of AZ-1355 differs from that of clofibrate.
D000818:Animals; D002784:Cholesterol / Q000097:blood; D002994:Clofibrate / Q000494:pharmacology; D006224:Cricetinae; D003989:Dibenzoxazepines / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D000960:Hypolipidemic Agents / Q000494:pharmacology*; D008074:Lipoproteins / Q000097:blood; D008099:Liver / Q000032:analysis; D008297:Male; D008647:Mesocricetus; D051379:Mice; D008815:Mice, Inbred Strains; D051381:Rats; D011919:Rats, Inbred Strains; D014280:Triglycerides / Q000097:blood
D003989:Dibenzoxazepines; D000960:Hypolipidemic Agents; D008074:Lipoproteins; D014280:Triglycerides; C033610:11,12-dihydro-4-methoxydibenz(b,f)(1,4)oxazepine-8-carboxylate; D002784:Cholesterol; D002994:Clofibrate