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Hypolipidemic effects in dogs of ML-236B, a competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase.

Abstract：

:ML-236B, a competitive inhibitor of 3-hydroxy-3-methylglutaryl-CoA reductase, significantly reduced both serum cholesterol and phospholipid levels in dogs, when used at a dosage higher than 10 mg/kg per day. Triglyceride levels were not consistently changed, but beta- and pre-beta-lipoproteins were preferentially reduced. Serum cholesterol levels were reduced by 44--45% at the higher dosage of 100--400 mg/kg per day (for 5 weeks) but ML-236B caused no significant changes in the cholesterol content of the liver and aorta and in the activities of serum GOT, GPT, CPK and lecithin : cholesterol acyltransferase. Fecal excretion of neutral sterols was unaffected but that of bile acids was markedly elevated by the drug. Under these conditions, hepatic cholesterol 7alpha-hydroxylase, the rate-limiting enzyme in bile acid biosynthesis, showed no detectable changes.

journal_name

Atherosclerosis

journal_title

Atherosclerosis

authors

Tsujita Y,Kuroda M,Tanzawa K,Kitano N,Endo A

doi

10.1016/0021-9150(79)90174-6

subject

Has Abstract

pub_date

1979-03-01 00:00:00

pages

307-13

issue

3

eissn

0021-9150

issn

1879-1484

pii

0021-9150(79)90174-6

journal_volume

32

pub_type

杂志文章

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