Cell-specific down-regulation of the beta 3-adrenergic receptor

J Biol Chem. 1994 May 6;269(18):13148-55.

Abstract

Previous studies have shown that beta 3-adrenergic receptors, in contrast to the beta 1 and beta 2 subtypes, do not undergo desensitization following short term activation (minutes) with agonists. Longer activation (hours) has been shown to induce desensitization of the beta 3-adrenergic receptor in some, but not all, cases, suggesting that cell- or species-specific mechanisms may be involved. We investigated the contribution of the cell type to the pattern of beta 3-adrenergic receptor long term desensitization by studying, in parallel, two cell lines (Chinese hamster fibroblasts and murine Ltk- cells) expressing the human beta 3-adrenergic receptor. Sustained agonist-promoted down-regulation of the beta 3-adrenergic receptor could be induced in Ltk- cells, whereas only a transient and weak reduction of receptor number was observed in Chinese hamster fibroblasts. The half-life of the beta 3-adrenergic receptor was not affected by the agonist activation in either cell line, indicating that in contrast to the beta 2-adrenergic receptor, degradation of preexisting receptor protein does not contribute to down-regulation. Sustained reduction of receptor RNA levels, monitored by reverse transcriptase polymerase chain reaction, was exclusively shown in Ltk- cells and probably accounted for most of the observed down-regulation. Differences in the ability of the receptor to stimulate adenylyl cyclase activity in the two cell lines may be responsible for the distinct patterns of beta 3-adrenergic receptor down-regulation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenylyl Cyclases / metabolism
  • Animals
  • Base Sequence
  • Cells, Cultured
  • Cricetinae
  • Cricetulus
  • Cyclic AMP / metabolism
  • Down-Regulation*
  • Enzyme Activation
  • Half-Life
  • Humans
  • Isoproterenol / pharmacology
  • Mice
  • Molecular Sequence Data
  • Oligodeoxyribonucleotides
  • RNA, Messenger / metabolism
  • Receptors, Adrenergic, beta / drug effects
  • Receptors, Adrenergic, beta / genetics
  • Receptors, Adrenergic, beta / metabolism*
  • Receptors, Adrenergic, beta-3

Substances

  • Oligodeoxyribonucleotides
  • RNA, Messenger
  • Receptors, Adrenergic, beta
  • Receptors, Adrenergic, beta-3
  • Cyclic AMP
  • Adenylyl Cyclases
  • Isoproterenol