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Inhibition of myocardial lipoprotein lipase by U-57,908 (RHC 80267)

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Lipids

Abstract

U-57,908 (RHC 80267) was shown to inhibit lipoprotein lipase (LPL) activity in cardiac myocytes from rat hearts; the concentrations required for inhibition to 50% of control activity were 1.1 μM and 2.5 μM for myocyte homogenates and a post-heparin medium preparation, respectively. The inhibition of LPL activity by U-57,908 was not changed when the concentration of the triolein substrate and apolipoprotein CII activator in the assay was reduced. The availability of U-57,908 as a potent and selective LPL inhibitor may provide a useful experimental approach in studies on lipoprotein metabolism.

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Abbreviations

DAG:

diacylglycerol

EDTA:

ethylenediaminetetraacetic acid

HEPES:

N-(2-hydroxyethyl)piperazine-N′(2-ethanesulfonic acid)

LPL:

lipoprotein lipase

PIPES:

piperazine-N,N′-bis(2-ethanesulfonic acid)

U-57,908:

cyclohexanone-O,O′[(1,6-hexanediyl)-bis(iminocarbonyl)]dioxime

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Authors and Affiliations

  1. MRC Signal Transduction Group, Faculty of Medicine, The University of Calgary, T2N 4N1, Calgary, Alberta, Canada

    Rogayah Carroll & David L. Severson

Authors
  1. Rogayah Carroll
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  2. David L. Severson
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Carroll, R., Severson, D.L. Inhibition of myocardial lipoprotein lipase by U-57,908 (RHC 80267). Lipids 27, 305–307 (1992). https://doi.org/10.1007/BF02536481

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  • DOI: https://doi.org/10.1007/BF02536481

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