Literature DB >> 21750562

Validation and quantification of [18F]altanserin binding in the rat brain using blood input and reference tissue modeling.

Patrick J Riss1, Young T Hong, David Williamson, Daniele Caprioli, Sergey Sitnikov, Valentina Ferrari, Steve J Sawiak, Jean-Claude Baron, Jeffrey W Dalley, Tim D Fryer, Franklin I Aigbirhio.   

Abstract

The 5-hydroxytryptamine type 2a (5-HT(2A)) selective radiotracer [(18)F]altanserin has been subjected to a quantitative micro-positron emission tomography study in Lister Hooded rats. Metabolite-corrected plasma input modeling was compared with reference tissue modeling using the cerebellum as reference tissue. [(18)F]altanserin showed sufficient brain uptake in a distribution pattern consistent with the known distribution of 5-HT(2A) receptors. Full binding saturation and displacement was documented, and no significant uptake of radioactive metabolites was detected in the brain. Blood input as well as reference tissue models were equally appropriate to describe the radiotracer kinetics. [(18)F]altanserin is suitable for quantification of 5-HT(2A) receptor availability in rats.

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Year:  2011        PMID： 21750562      PMCID： PMC3323196          DOI： 10.1038/jcbfm.2011.94

Source DB:  PubMed          Journal:  J Cereb Blood Flow Metab        ISSN： 0271-678X            Impact factor:   6.200


  32 in total

1.  5-HT2A receptor gene promoter polymorphism -1438A/G and bipolar disorder.

Authors:  I S Chee; S W Lee; J L Kim; S K Wang; Y O Shin; S C Shin; Y H Lee; H M Hwang; M R Lim
Journal:  Psychiatr Genet       Date:  2001-09       Impact factor: 2.458

2.  In vivo binding of [18F]altanserin to rat brain 5HT2 receptors: a film and electronic autoradiographic study.

Authors:  F Biver; F Lotstra; M Monclus; S Dethy; P Damhaut; D Wikler; A Luxen; S Goldman
Journal:  Nucl Med Biol       Date:  1997-05       Impact factor: 2.408

3.  Binding characteristics of the 5-HT2A receptor antagonists altanserin and MDL 100907.

Authors:  Heidi Kristiansen; Betina Elfving; Per Plenge; Lars H Pinborg; Nic Gillings; Gitte M Knudsen
Journal:  Synapse       Date:  2005-12-15       Impact factor: 2.562

4.  Association between schizophrenia and T102C polymorphism of the 5-hydroxytryptamine type 2a-receptor gene. European Multicentre Association Study of Schizophrenia (EMASS) Group.

Authors:  J Williams; G Spurlock; P McGuffin; J Mallet; M M Nöthen; M Gill; H Aschauer; P O Nylander; F Macciardi; M J Owen
Journal:  Lancet       Date:  1996-05-11       Impact factor: 79.321

5.  Characterization of radioactive metabolites of 5-HT2A receptor PET ligand [18F]altanserin in human and rodent.

Authors:  P Z Tan; R M Baldwin; C H Van Dyck; M Al-Tikriti; B Roth; N Khan; D S Charney; R B Innis
Journal:  Nucl Med Biol       Date:  1999-08       Impact factor: 2.408

Review 6.  Measuring endogenous 5-HT release by emission tomography: promises and pitfalls.

Authors:  Louise M Paterson; Robin J Tyacke; David J Nutt; Gitte M Knudsen
Journal:  J Cereb Blood Flow Metab       Date:  2010-07-28       Impact factor: 6.200

7.  Test-retest variability of serotonin 5-HT2A receptor binding measured with positron emission tomography and [18F]altanserin in the human brain.

Authors:  G S Smith; J C Price; B J Lopresti; Y Huang; N Simpson; D Holt; N S Mason; C C Meltzer; R A Sweet; T Nichols; D Sashin; C A Mathis
Journal:  Synapse       Date:  1998-12       Impact factor: 2.562

8.  Multicompartmental study of fluorine-18 altanserin binding to brain 5HT2 receptors in humans using positron emission tomography.

Authors:  F Biver; S Goldman; A Luxen; M Monclus; M Forestini; J Mendlewicz; F Lotstra
Journal:  Eur J Nucl Med       Date:  1994-09

9.  Distribution volume ratios without blood sampling from graphical analysis of PET data.

Authors:  J Logan; J S Fowler; N D Volkow; G J Wang; Y S Ding; D L Alexoff
Journal:  J Cereb Blood Flow Metab       Date:  1996-09       Impact factor: 6.200

10.  Fluorine-18-altanserin: a radioligand for the study of serotonin receptors with PET: radiolabeling and in vivo biologic behavior in rats.

Authors:  C Lemaire; R Cantineau; M Guillaume; A Plenevaux; L Christiaens
Journal:  J Nucl Med       Date:  1991-12       Impact factor: 10.057
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  6 in total

Review 1.  Quantitative Rodent Brain Receptor Imaging.

Authors:  Kristina Herfert; Julia G Mannheim; Laura Kuebler; Sabina Marciano; Mario Amend; Christoph Parl; Hanna Napieczynska; Florian M Maier; Salvador Castaneda Vega; Bernd J Pichler
Journal:  Mol Imaging Biol       Date:  2020-04       Impact factor: 3.488

2.  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

3.  Insula serotonin 2A receptor binding and gene expression contribute to serotonin transporter polymorphism anxious phenotype in primates.

Authors:  Andrea M Santangelo; Steve J Sawiak; Tim Fryer; Young Hong; Yoshiro Shiba; Hannah F Clarke; Patrick J Riss; Valentina Ferrari; Roger Tait; John Suckling; Franklin I Aigbirhio; Angela C Roberts
Journal:  Proc Natl Acad Sci U S A       Date:  2019-07-02       Impact factor: 11.205

4.  Radioligand binding analysis of α 2 adrenoceptors with [11C]yohimbine in brain in vivo: Extended Inhibition Plot correction for plasma protein binding.

Authors:  Jenny-Ann Phan; Anne M Landau; Steen Jakobsen; Dean F Wong; Albert Gjedde
Journal:  Sci Rep       Date:  2017-11-22       Impact factor: 4.379

5.  Pharmacological Characterization of Low-to-Moderate Affinity Opioid Receptor Agonists and Brain Imaging with 18F-Labeled Derivatives in Rats.

Authors:  Julian Ott; Mona M Spilhaug; Simone Maschauer; Waqas Rafique; Jimmy E Jakobsson; Karoline Hartvig; Harald Hübner; Peter Gmeiner; Olaf Prante; Patrick J Riss
Journal:  J Med Chem       Date:  2020-08-17       Impact factor: 7.446

6.  Kinetic analysis of [18F] altanserin bolus injection in the canine brain using PET imaging.

Authors:  Glenn Pauwelyn; Lise Vlerick; Robrecht Dockx; Jeroen Verhoeven; Andre Dobbeleir; Tim Bosmans; Kathelijne Peremans; Christian Vanhove; Ingeborgh Polis; Filip De Vos
Journal:  BMC Vet Res       Date:  2019-11-21       Impact factor: 2.741
  6 in total

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