PMID: 11323237Apr 27, 2001Paper

Comparison of [(18)F]altanserin and [(18)F]deuteroaltanserin for PET imaging of serotonin(2A) receptors in baboon brain: pharmacological studies

Nuclear Medicine and Biology
J K StaleyR B Innis

Abstract

The regional distribution in brain, distribution volumes, and pharmacological specificity of the PET 5-HT(2A) receptor radiotracer [(18)F]deuteroaltanserin were evaluated and compared to those of its non-deuterated derivative [(18)F]altanserin. Both radiotracers were administered to baboons by bolus plus constant infusion and PET images were acquired up to 8 h. The time-activity curves for both tracers stabilized between 4 and 6 h. The ratio of total and free parent to metabolites was not significantly different between radiotracers; nevertheless, total cortical R(T) (equilibrium ratio of specific to nondisplaceable brain uptake) was significantly higher (34-78%) for [(18)F]deuteroaltanserin than for [(18)F]altanserin. In contrast, the binding potential (Bmax/K(D)) was similar between radiotracers. [(18)F]Deuteroaltanserin cortical activity was displaced by the 5-HT(2A) receptor antagonist SR 46349B but was not altered by changes in endogenous 5-HT induced by fenfluramine. These findings suggest that [(18)F]deuteroaltanserin is essentially equivalent to [(18)F]altanserin for 5-HT(2A) receptor imaging in the baboon.

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Citations

Feb 24, 2007·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Nicolaas I Bohnen, Kirk A Frey
Dec 5, 2009·Psychiatry Research·Paul H SoloffCarolyn C Meltzer
Jul 29, 2010·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·Louise M PatersonGitte M Knudsen
Apr 30, 2015·Psychopharmacology·Sjoerd J FinnemaSarah Grimwood
Aug 7, 2003·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·Lars H PinborgGitte M Knudsen
Sep 10, 2004·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·Lars H PinborgGitte M Knudsen
Dec 3, 2008·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Stina SyvänenMargareta Hammarlund-Udenaes
Nov 13, 2019·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·David ErritzoeEugenii A Rabiner
Jun 16, 2011·Medicinal Research Reviews·Louise M PatersonGitte M Knudsen
Nov 23, 2019·BMC Veterinary Research·Glenn PauwelynFilip De Vos
Apr 5, 2020·Nuclear Medicine and Biology·Zhihao ZhaHank F Kung

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