Serotonin concentration enhancers at clinically relevant doses reduce [11 C]AZ10419369 binding to the 5-HT1B receptors in the nonhuman primate brain

Translational Psychiatry
Kai-Chun YangSjoerd J Finnema

Abstract

The serotonin (5-HT) system plays an important role in the pathophysiology and treatment of several major psychiatric disorders. Currently, no suitable positron emission tomography (PET) imaging paradigm is available to assess 5-HT release in the living human brain. [11C]AZ10419369 binds to 5-HT1B receptors and is one of the most 5-HT-sensitive radioligands available. This study applied 5-HT concentration enhancers which can be safely studied in humans, and examined their effect on [11C]AZ10419369 binding at clinically relevant doses, including amphetamine (1 mg/kg), 3,4-methylenedioxymethamphetamine (MDMA; 1 mg/kg) or 5-hydroxy-L-tryptophan (5-HTP; 5 mg/kg). Twenty-six PET measurements (14 for amphetamine, 6 for MDMA and 6 for 5-HTP) using a bolus and constant infusion protocol were performed in four cynomolgus monkeys before or after drug administration. Binding potential (BPND) values were determined with the equilibrium method (integral interval: 63-123 min) using cerebellum as the reference region. BPND values were significantly decreased in several examined brain regions after administration of amphetamine (range: 19-31%), MDMA (16-25%) or 5-HTP (13-31%). Reductions in [11C]AZ10419369 binding were greater in striatum than...Continue Reading

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Citations

Jun 20, 2019·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Kai-Chun YangSjoerd J Finnema
Sep 22, 2019·European Journal of Nuclear Medicine and Molecular Imaging·Stuart P McCluskeyOliver Howes
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Jun 7, 2019·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Kristina HerfertBernd J Pichler
Mar 26, 2021·Frontiers in Neuroscience·Matthieu ColomLuc Zimmer
Aug 1, 2021·Drug Discovery Today·Krishna Kanta GhoshBalázs Gulyás

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GraphPad
PMOD Fuse It Tool ( PFUSEIT )
Image Processing and VOI Analysis Tool ( PBAS )
GraphPad Prism
antsRegistration
PMOD
Advanced Normalization Tools ( ANTs )
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