Differential sensitivity of [3H]7-OH-DPAT-labeled binding sites in rat brain to inactivation by N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline

Brain Research
B Levant

Abstract

The effects of alkylating agent N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ) on the binding of [3H]7-OH-DPAT, a ligand for the D3 dopamine receptor, were assessed in ventral striatal (n. accumbens and olf. tubercle) membranes of adult, male Sprague-Dawley rats. [3H]Spiperone binding to D2-like receptors in striatal membranes was also assayed as a positive control. In vitro, EEDQ was equipotent in inactivating [3H]7-OH-DPAT- and [3H]spiperone-labeled binding sites. In vitro, [3H]spiperone binding was rapidly eliminated in a dose-dependent manner following EEDQ administration. In contrast, [3H]7-OH-DPAT binding was not significantly altered by any dose of the alkylating agent at any time point examined. Depletion of endogenous catecholamines with alpha-methyltyrosine and reserpine revealed a second, higher affinity binding site for [3H]7-OH-DPAT. Administration of EEDQ in catecholamine-depleted animals reduced [3H]7-OH-DPAT labels two distinct populations of binding binding sites in rat brain membranes, only one of which is susceptible to inactivation by EEDQ. These sites may represent high and low affinity states of the D3 receptor. In addition, this discovery may provide a useful method for examining the function of so...Continue Reading

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Citations

Jun 3, 1996·European Journal of Pharmacology·C W Aretha, M P Galloway
Feb 26, 2005·Journal of Clinical Psychology·Glenn E GoodAllyson D Brathwaite
Mar 29, 2005·The American Journal of Orthopsychiatry·Wilma J Lutz, Ellen Hock
Jun 1, 1997·Gender and Development·N Sampath
Oct 25, 2012·American Journal of Men's Health·William AffleckMary Ellen Macdonald
Dec 8, 2005·Trauma, Violence & Abuse·Mudita Rastogi, Paul Therly
Dec 30, 2009·American Journal of Men's Health·David S Shen-MillerTimothy Boling
Apr 5, 2003·The American Psychologist·Michael E Addis, James R Mahalik
Sep 1, 2017·Journal of Central Nervous System Disease·G Aleph Prieto
Oct 13, 2018·American Journal of Men's Health·Brian P ColeAshley Kuznia
Nov 4, 2004·Journal of Receptor and Signal Transduction Research·Joy A Ahlgren-Beckendorf, Beth Levant

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