Multiple mechanisms of CB1 cannabinoid receptors regulation.
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.
Keren
Ora
O
The Mauerberger Chair in Neuropharmacology, Department of Physiology and Pharmacology, Sackler Faculty of Medicine, Tel-Aviv University, Tel-Aviv 69978, Israel.
Sarne
Yosef
Y
D000818:Animals; D002186:Cannabinoids / Q000378:metabolism* / Q000494:pharmacology; D002460:Cell Line; D015536:Down-Regulation / Q000187:drug effects / Q000502:physiology*; D004705:Endocytosis / Q000187:drug effects / Q000502:physiology; D006801:Humans; D051379:Mice; D011485:Protein Binding / Q000187:drug effects / Q000502:physiology; D043882:Receptors, Cannabinoid; D011955:Receptors, Drug / Q000819:agonists / Q000378:metabolism*; D014407:Tumor Cells, Cultured
D002186:Cannabinoids; D043882:Receptors, Cannabinoid; D011955:Receptors, Drug