Inhibition of the rat renal Na+/H+ exchanger by beta-adrenergic antagonists

Biochem Biophys Res Commun. 1991 Feb 28;175(1):311-7. doi: 10.1016/s0006-291x(05)81236-7.

Abstract

The beta-adrenergic antagonists, alprenolol and propranolol, inhibit the Na+/H+ exchanger in rat renal brush-border membrane vesicles. Half-maximal inhibition occurs at 86 microM alprenolol and 36 microM propranolol. Similar to amiloride and Na+, propranolol protects the Na+/H+ exchanger from irreversible inhibition by the carboxyl group reagent, N,N'-dicyclohexyl-carbodiimide (DCCD). Protection is incomplete, depends on propranolol concentration, and reaches a maximum at 0.4 mM propranolol. With a comparable dose dependence, propranolol protects a 65 kDa band from labeling with [14C]DCCD. The data indicate that beta-adrenergic antagonists specifically interact with the proximal tubular Na+/H+ exchanger.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adrenergic beta-Antagonists / pharmacology*
  • Alprenolol / pharmacology*
  • Amiloride / pharmacology
  • Animals
  • Carrier Proteins / antagonists & inhibitors*
  • Carrier Proteins / isolation & purification
  • Dicyclohexylcarbodiimide / metabolism
  • Dicyclohexylcarbodiimide / pharmacology
  • Dose-Response Relationship, Drug
  • Kidney Cortex / metabolism*
  • Kinetics
  • Microvilli / metabolism
  • Pindolol / pharmacology
  • Propranolol / pharmacology*
  • Protein Binding
  • Rats
  • Sodium-Hydrogen Exchangers

Substances

  • Adrenergic beta-Antagonists
  • Carrier Proteins
  • Sodium-Hydrogen Exchangers
  • Dicyclohexylcarbodiimide
  • Amiloride
  • Alprenolol
  • Propranolol
  • Pindolol