Block of neurotensin receptor down-regulation by an aminosteroid in N1E-115 cells.
We have demonstrated that the aminosteroid, U-73122 (1-(6-([17 beta-3-methoxyestra-1,3,5(10)-trien-17-yl]amino)hexyl)-1H-pyrrole- 2,5-dione) blocks agonist induced down-regulation of neurotensin receptors in murine neuroblastoma clone N1E-115 cells. U-73122 is known to inhibit polyphosphoinositide hydrolysis by affecting the coupling of GTP-binding proteins. Our results may indicate that GTP-binding proteins play a role in the mechanism of down-regulation of the neurotensin receptor.
Yamada
M
M
Mayo Foundation, Jacksonville, FL 32224.
Yamada
M
M
Richelson
E
E
D015536:Down-Regulation / Q000187:drug effects*; D004963:Estrenes / Q000494:pharmacology*; D019204:GTP-Binding Proteins / Q000378:metabolism; D009447:Neuroblastoma / Q000378:metabolism; D009496:Neurotensin / Q000494:pharmacology; D011760:Pyrrolidinones / Q000494:pharmacology*; D011976:Receptors, Muscarinic / Q000187:drug effects; D018028:Receptors, Neurotensin; D017981:Receptors, Neurotransmitter / Q000037:antagonists & inhibitors*; D014407:Tumor Cells, Cultured; D010738:Type C Phospholipases / Q000037:antagonists & inhibitors*
D004963:Estrenes; D011760:Pyrrolidinones; D011976:Receptors, Muscarinic; D018028:Receptors, Neurotensin; D017981:Receptors, Neurotransmitter; C060229:1-(6-((3-methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl)-1H-pyrrole-2,5-dione; D009496:Neurotensin; D010738:Type C Phospholipases; D019204:GTP-Binding Proteins