In vivo [11C]dihydrotetrabenazine binding in rat striatum: sensitivity to dopamine concentrations.

Nuclear Medicine and Biology
M R KilbournK A Frey

Abstract

The sensitivity of the in vivo binding of [(11)C]dihydrotetrabenazine ([(11)C]DTBZ) and [(11)C]methylphenidate ([(11)C]MPH) to their respective targets - vesicular monoamine transporter type 2 (VMAT2) and neuronal membrane dopamine transporter - after alterations in endogenous levels of dopamine was examined in the rat brain. In vivo binding of [(11)C]DTBZ and [(11)C]MPH was determined using a bolus+infusion protocol. The in vitro number of VMAT2 binding sites was determined by autoradiography. Repeated dosing with alpha-methyl-p-tyrosine (AMPT) at doses that significantly (-75%) depleted brain tissue dopamine levels resulted in increased (+36%) in vivo [(11)C]DTBZ binding to VMAT2 in the striatum. The increase in binding could be completely reversed via treatment with L-DOPA/benserazide to restore dopamine levels. There were no changes in the total number of VMAT2 binding sites, as measured using in vitro autoradiography. No changes were observed for in vivo [(11)C]MPH binding to the dopamine transporter in the striatum following AMPT pretreatment. These results indicate that large reductions in dopamine concentrations in the rat brain can produce modest but significant changes in the binding of radioligands to VMAT2, which ca...Continue Reading

References

Jun 1, 1989·Biochemical Pharmacology·N T Buu
Feb 1, 1997·Nuclear Medicine and Biology·D M JewettL C Lee
Apr 24, 2003·Synapse·Raúl De La Fuente-FernándezA Jon Stoessl
Apr 25, 2009·Synapse·Raúl de la Fuente-FernándezA Jon Stoessl

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Citations

Sep 7, 2012·Diabetes, Obesity & Metabolism·P E Harris, R L Leibel
Sep 1, 2015·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Isabelle BoileauStephen J Kish
Apr 28, 2011·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·Junchao TongStephen J Kish
Jan 29, 2011·Annals of the New York Academy of Sciences·Lee E Eiden, Eberhard Weihe
Sep 16, 2015·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Matthew J FreebyPaul E Harris
Feb 14, 2012·Neuro-degenerative Diseases·Anne M LandauDoris J Doudet
May 8, 2018·Zeitschrift für Gerontologie und Geriatrie·Jennifer Fietz, Barbara Stupp
Sep 4, 2019·Diabetes, Obesity & Metabolism·Kyoungjune PakIn Joo Kim

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