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Subsensitivity of adenylate cyclase and decreased beta-adrenergic receptor binding after chronic exposure to (minus)-isoproterenol in vitro.

Publication ,  Journal Article
Mickey, J; Tate, R; Lefkowitz, RJ
Published in: J Biol Chem
July 25, 1975

In vitro incubation of frog erythrocytes with (minus)-isoproterenol, 0.1 mM, at 23 degrees for 10 to 24 hours caused a 63% decline (rho less than 0.001) in the maximum (minus)-isoproterenol-stimulated adenylate cyclase activity in the erythrocyte membranes. Affinity for (minus)-isoproterenol as judged by the concentration which half-maximally stimulated the enzyme was not markedly altered. Basal enzyme activity and stimulation by fluoride or prostaglandin E1 remained unaltered. The number of beta-adrenergic receptor binding sites, assessed by binding studies with the beta-adrenergic antagonist (minus)-[3-H] alprenolol, declined by 50% (rho less than 0.005) in the (minus)-isoproterenol-treated cells. The binding affinity of the sites was not changed. Regulation of the concentration of functionally active beta-adrenergic receptors in membranes may be one of the mechanisms by which chronic exposure to catecholamines desensitizes tissues to beta-adrenergic stimulation.

Duke Scholars

Published In

J Biol Chem

ISSN

0021-9258

Publication Date

July 25, 1975

Volume

250

Issue

14

Start / End Page

5727 / 5729

Location

United States

Related Subject Headings

  • Tritium
  • Receptors, Cell Surface
  • Receptors, Adrenergic
  • Prostaglandins E
  • Myocardium
  • Membranes
  • Ligands
  • Isoproterenol
  • In Vitro Techniques
  • Erythrocytes
 

Published In

J Biol Chem

ISSN

0021-9258

Publication Date

July 25, 1975

Volume

250

Issue

14

Start / End Page

5727 / 5729

Location

United States

Related Subject Headings

  • Tritium
  • Receptors, Cell Surface
  • Receptors, Adrenergic
  • Prostaglandins E
  • Myocardium
  • Membranes
  • Ligands
  • Isoproterenol
  • In Vitro Techniques
  • Erythrocytes