Literature DB >> 20083209

Simplified quantification of 5-HT2A receptors in the human brain with [11C]MDL 100,907 PET and non-invasive kinetic analyses.

Philipp T Meyer1, Zubin Bhagwagar, Philip J Cowen, Vincent J Cunningham, Paul M Grasby, Rainer Hinz.   

Abstract

BACKGROUND: [(11)C]MDL100,907 is a promising positron emission tomography (PET) ligand for 5-HT(2A) receptor quantification in vivo. Studies suggest that [(11)C]MDL100,907 PET may be quantified by non-invasive reference tissue analyses using cerebellum as reference region. We systematically investigated the validity of such analyses.
METHODS: Five healthy volunteers underwent [(11)C]MDL100,907 PET at baseline and after mirtazapine pre-treatment. Regional time-activity curves of 10 regions of interest (ROI) were analyzed for binding potential (BP(ND)) and mirtazapine receptor occupancy (Occ) using: simplified reference tissue model (SRTM), multi-linear reference tissue model (MRTM), their two-parameter versions (SRTM2/MRTM2), non-invasive graphical analysis (NIGA) and a tissue activity concentration ratio. NIGA was also applied voxel-wise to generate BP(ND) maps. These methods were compared with a two-tissue compartment model with arterial input function (2TCM)
Results: SRTM and MRTM frequently failed to yield reliable results. SRTM2 and MRTM2 gave virtually identical estimates of BP(ND), which were highly correlated with 2TCM analyses (R(2)>or=0.86) although with negative bias (-29+/-27% at baseline across all ROI). NIGA was less biased (-19+/-16%) and better correlated with 2TCM (R(2)>or=0.93). Regarding Occ, NIGA and SRTM2/MRTM2 showed comparable mean biases (-11+/-27% vs. -7+/-47%) but correlation with 2TCM was higher for NIGA (R(2)=0.90 vs. 0.77). NIGA parametric maps (analysed using identical ROI) resulted in moderate bias in BP(ND) (-26+/-22%; R(2)>or=0.88) and Occ (-17+/-36%; R(2)=0.78). Estimates obtained from tissue ratios performed least favourably.
CONCLUSIONS: NIGA is well suited for analysis of [(11)C]MDL100,907 PET studies, yielding estimates of 5-HT(2A) receptor availability and changes that are highly correlated with results from invasive 2TCM analyses. This should greatly enhance the applicability of 5-HT(2A) receptor PET studies. Copyright 2010 Elsevier Inc. All rights reserved.

Entities:  

Mesh:

Substances:

Year:  2010        PMID: 20083209     DOI: 10.1016/j.neuroimage.2010.01.037

Source DB:  PubMed          Journal:  Neuroimage        ISSN: 1053-8119            Impact factor:   6.556


  10 in total

1.  Brain serotonergic circuitries.

Authors:  Yves Charnay; Lucienne Léger
Journal:  Dialogues Clin Neurosci       Date:  2010       Impact factor: 5.986

2.  Analysis of 5-HT(2A) receptor binding with [(11)C]MDL 100907 in rats: optimization of kinetic modeling.

Authors:  Anniek K D Visser; Erik F J De Vries; Nisha K Ramakrishnan; Antoon T M Willemsen; Fokko J Bosker; Johan A den Boer; Rudi A J O Dierckx; Aren van Waarde
Journal:  Mol Imaging Biol       Date:  2013-12       Impact factor: 3.488

3.  Synthesis and imaging validation of [¹⁸F]MDL100907 enabled by Ni-mediated fluorination.

Authors:  Hong Ren; Hsiao-Ying Wey; Martin Strebl; Ramesh Neelamegam; Tobias Ritter; Jacob M Hooker
Journal:  ACS Chem Neurosci       Date:  2014-06-03       Impact factor: 4.418

4.  Characterization of the serotonin 2A receptor selective PET tracer (R)-[18F]MH.MZ in the human brain.

Authors:  Vasko Kramer; Agnete Dyssegaard; Jonathan Flores; Cristian Soza-Ried; Frank Rösch; Gitte Moos Knudsen; Horacio Amaral; Matthias M Herth
Journal:  Eur J Nucl Med Mol Imaging       Date:  2019-10-12       Impact factor: 9.236

5.  Radiosynthesis and in vivo evaluation of a series of substituted 11C-phenethylamines as 5-HT (2A) agonist PET tracers.

Authors:  Anders Ettrup; Martin Hansen; Martin A Santini; James Paine; Nic Gillings; Mikael Palner; Szabolcs Lehel; Matthias M Herth; Jacob Madsen; Jesper Kristensen; Mikael Begtrup; Gitte M Knudsen
Journal:  Eur J Nucl Med Mol Imaging       Date:  2010-12-21       Impact factor: 9.236

6.  Serotonin 2A receptor agonist binding in the human brain with [¹¹C]Cimbi-36.

Authors:  Anders Ettrup; Sophie da Cunha-Bang; Brenda McMahon; Szabolcs Lehel; Agnete Dyssegaard; Anine W Skibsted; Louise M Jørgensen; Martin Hansen; Anders O Baandrup; Søren Bache; Claus Svarer; Jesper L Kristensen; Nic Gillings; Jacob Madsen; Gitte M Knudsen
Journal:  J Cereb Blood Flow Metab       Date:  2014-04-30       Impact factor: 6.200

7.  Extended characterisation of the serotonin 2A (5-HT2A) receptor-selective PET radiotracer 11C-MDL100907 in humans: quantitative analysis, test-retest reproducibility, and vulnerability to endogenous 5-HT tone.

Authors:  Peter S Talbot; Mark Slifstein; Dah-Ren Hwang; Yiyun Huang; Erica Scher; Anissa Abi-Dargham; Marc Laruelle
Journal:  Neuroimage       Date:  2011-07-18       Impact factor: 6.556

8.  Suitability of [18F]altanserin and PET to determine 5-HT2A receptor availability in the rat brain: in vivo and in vitro validation of invasive and non-invasive kinetic models.

Authors:  Tina Kroll; David Elmenhorst; Andreas Matusch; Franziska Wedekind; Angela Weisshaupt; Simone Beer; Andreas Bauer
Journal:  Mol Imaging Biol       Date:  2013-03-01       Impact factor: 3.488

Review 9.  5-HT radioligands for human brain imaging with PET and SPECT.

Authors:  Louise M Paterson; Birgitte R Kornum; David J Nutt; Victor W Pike; Gitte M Knudsen
Journal:  Med Res Rev       Date:  2011-06-14       Impact factor: 12.944

10.  Fenfluramine Reduces [11C]Cimbi-36 Binding to the 5-HT2A Receptor in the Nonhuman Primate Brain.

Authors:  Kai-Chun Yang; Vladimir Stepanov; Stefan Martinsson; Anders Ettrup; Akihiro Takano; Gitte M Knudsen; Christer Halldin; Lars Farde; Sjoerd J Finnema
Journal:  Int J Neuropsychopharmacol       Date:  2017-09-01       Impact factor: 5.176

  10 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.