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Decrease in enkephalinase A number in kidney membranes from hypercholesterolemic and hypertensive rats.

M P Fournet-Bourguignon1, S Illiano, A Lenaers

  • 1Groupe de Recherches Servier, FONDAX ACTAM et CIE, Puteaux, France.

Journal of Receptor Research
|January 1, 1992
PubMed
Summary
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Enkephalinase A levels decrease in rat kidneys with hypertension and hypercholesterolemia. This study quantifies these changes, offering insights into peptidic substrate metabolism in these conditions.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Nephrology

Background:

  • Enkephalinase A plays a role in peptidic substrate metabolism.
  • Hypertension and hypercholesterolemia are conditions affecting kidney function.

Purpose of the Study:

  • To investigate the variation of enkephalinase A in rat kidney membranes under hypertensive and hypercholesterolemic conditions.
  • To quantify the binding characteristics of [3H]-acetorphan to rat kidney membranes.

Main Methods:

  • Utilized [3H]-acetorphan, a potent enkephalinase A inhibitor, to label the protease in rat kidney membranes.
  • Employed equilibrium and kinetic binding assays to determine in vitro binding characteristics.
  • Compared binding capacity in Sprague Dawley and Wistar Kyoto rat kidney membranes.

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Main Results:

  • [3H]-acetorphan binding to kidney membranes is saturable, reversible, and involves a single class of sites (Kd = 4-5.3 nM).
  • Enkephalinase A binding capacity (Bmax ≈ 51 pmol/mg protein) was consistent across rat strains.
  • Enkephalinase A levels decreased by 20% in hypertensive rats and 50% in hypercholesterolemic rats.

Conclusions:

  • Hypertension and hypercholesterolemia are associated with a significant reduction in renal enkephalinase A.
  • These findings suggest alterations in peptidic substrate metabolism in the diseased kidney states.