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High Volume Screening Procedures for Hypobetalipoproteinemic Activity in Rats

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Atherosclerosis Drug Discovery

Part of the book series: Advances in Experimental Medicine and Biology ((AEMB,volume 67))

Abstract

We describe high volume screening tests for hypobetalipoproteinemic agents in which compounds are administered orally to cholesterol-cholic acid fed (hypercholesterolemic) or normally fed weanling rats for 4 days. In these tests total serum cholesterol levels and heparin precipitating lipoproteins (HPL) are determined by automated analyses interfaced with a computer which eliminates all manual data reduction and provides necessary reports. The hypercholesterolemic rat test detects compounds which specifically reduce HPL (beta and pre beta lipoproteins) causing a decrease in the HPL:cholesterol ratio. Such activity is called hypobetalipoproteinemia. This activity is exhibited by bicyclo(2.2.2)-octyloxyaniline (U-26328) but not by any of the familiar hypocholesterolemic agents including clofibrate, lifibrate, nicotinic acid, probucol, triparanol, lentysine, D-thyroxine or the estrogens estrone and diethylstilbestrol.

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Schurr, P.E., Schultz, J.R., Day, C.E. (1976). High Volume Screening Procedures for Hypobetalipoproteinemic Activity in Rats. In: Day, C.E. (eds) Atherosclerosis Drug Discovery. Advances in Experimental Medicine and Biology, vol 67. Springer, Boston, MA. https://doi.org/10.1007/978-1-4614-4618-7_13

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  • DOI: https://doi.org/10.1007/978-1-4614-4618-7_13

  • Publisher Name: Springer, Boston, MA

  • Print ISBN: 978-1-4757-9309-3

  • Online ISBN: 978-1-4614-4618-7

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