Multiple mechanisms of CB1 cannabinoid receptors regulation

Brain Res. 2003 Aug 8;980(2):197-205. doi: 10.1016/s0006-8993(03)02970-6.

Abstract

Agonist-induced regulation of cannabinoid CB1 receptors was examined in HEK-293 cells transfected with CB1 receptors and in neuroblastoma N18TG2 cells that naturally express CB1 receptors. In HEK-293 cells, CB1 receptors internalization proceeded, in parallel, via clathrin-coated pits and caveolae. Simultaneous disruption of both pathways induced compensatory endocytic mechanism(s). In N18TG2 cells, endocytosis was not mediated by caveolae-like membrane domains. Heterologous, opioid-induced, downregulation of CB1 receptors was evident in HEK-293 but not N18TG2 cells. The data demonstrate the existence of multiple pathways of CB1 receptors regulation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cannabinoids / metabolism*
  • Cannabinoids / pharmacology
  • Cell Line
  • Down-Regulation / drug effects
  • Down-Regulation / physiology*
  • Endocytosis / drug effects
  • Endocytosis / physiology
  • Humans
  • Mice
  • Protein Binding / drug effects
  • Protein Binding / physiology
  • Receptors, Cannabinoid
  • Receptors, Drug / agonists
  • Receptors, Drug / metabolism*
  • Tumor Cells, Cultured

Substances

  • Cannabinoids
  • Receptors, Cannabinoid
  • Receptors, Drug