Studies on the intrinsic activity (efficacy) of human adrenergic receptors. Co-expression of beta 1 and beta 2 reveals a lower efficacy for the beta 1 receptor

Tex Heart Inst J. 1994;21(1):16-21.

Abstract

Through co-expression of the human beta 1 and beta 2 adrenergic receptors in a single tester cell (the murine L fibroblast) and through assaying the effect of the beta 1 and beta 2 selective blockers CGP 20712A and ICI 118551 on isoproterenol-stimulated adenylyl cyclase, it is shown that the maximal stimulation achievable with a given cell density of beta 1 adrenergic receptor is less than that obtained with the same density of the beta 2 adrenergic receptor. It is concluded that the efficacy of the 2 receptors differs in that the beta 1 adrenergic receptor has a lower efficacy (or intrinsic activity) than does the beta 2 adrenergic receptor.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adenylyl Cyclases / metabolism
  • Amino Acid Sequence
  • Animals
  • Cell Line
  • Humans
  • L Cells
  • Mice
  • Molecular Sequence Data
  • Myocardium / metabolism
  • Pindolol / analogs & derivatives
  • Pindolol / metabolism
  • Receptors, Adrenergic, beta / analysis*
  • Receptors, Adrenergic, beta / physiology*

Substances

  • Receptors, Adrenergic, beta
  • cyanopindolol
  • Pindolol
  • Adenylyl Cyclases