Literature DB >> 20021353

Imaging of sigma1 receptors in the human brain using PET and [11C]SA4503.

Jun Toyohara1, Muneyuki Sakata, Kiichi Ishiwata.   

Abstract

Sigma(1) receptors were imaged in living human brain by positron emission tomography (PET) using [(11)C] SA4503. A dynamic 90-min scan and kinetic analysis enabled quantification of receptor density in the brain. The sigma(1) receptors were distributed throughout the brain in normal subjects, but decreased in the frontal, temporal, and occipital lobes, cerebellum and thalamus in patients with early Alzheimer's disease and in the putamen in patients with Parkinson's disease. In addition, rates of receptor occupancy by the neuroleptic haloperidol and the selective serotonin reuptake inhibitor fluvoxamine were evaluated by [(11)C]SA4503-PET and found to be high. [(11)C]SA4503-PET is useful for studying the pathophysiology of neurological and psychiatric disorders such as schizophrenia and for evaluation of the pharmacodynamics of psychiatric drugs.

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Year:  2009        PMID: 20021353     DOI: 10.2174/1871524910909030190

Source DB:  PubMed          Journal:  Cent Nerv Syst Agents Med Chem        ISSN: 1871-5249


  18 in total

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3.  Imaging Sigma-1 Receptor (S1R) Expression Using Iodine-124-Labeled 1-(4-Iodophenyl)-3-(2-adamantyl)guanidine ([124I]IPAG).

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Journal:  Mol Imaging Biol       Date:  2020-04       Impact factor: 3.488

4.  Radiosynthesis and in vivo evaluation of a novel σ1 selective PET ligand.

Authors:  Hongjun Jin; Jinda Fan; Xiang Zhang; Junfeng Li; Hubert P Flores; Joel S Perlmutter; Stanley M Parsons; Zhude Tu
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5.  Sigma receptors [σRs]: biology in normal and diseased states.

Authors:  Colin G Rousseaux; Stephanie F Greene
Journal:  J Recept Signal Transduct Res       Date:  2015-06-09       Impact factor: 2.092

6.  Compromising σ-1 receptors at the endoplasmic reticulum render cytotoxicity to physiologically relevant concentrations of dopamine in a nuclear factor-κB/Bcl-2-dependent mechanism: potential relevance to Parkinson's disease.

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Journal:  J Pharmacol Exp Ther       Date:  2012-03-07       Impact factor: 4.030

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Authors:  James A Fishback; Christophe Mesangeau; Jacques H Poupaert; Christopher R McCurdy; Rae R Matsumoto
Journal:  Eur J Pharmacol       Date:  2010-12-02       Impact factor: 4.432

8.  Ether modifications to 1-[2-(3,4-dimethoxyphenyl)ethyl]-4-(3-phenylpropyl)piperazine (SA4503): effects on binding affinity and selectivity for sigma receptors and monoamine transporters.

Authors:  Rong Xu; Sarah A Lord; Ryan M Peterson; Emily A Fergason-Cantrell; John R Lever; Susan Z Lever
Journal:  Bioorg Med Chem       Date:  2014-11-11       Impact factor: 3.641

9.  New positron emission tomography (PET) radioligand for imaging σ-1 receptors in living subjects.

Authors:  Michelle L James; Bin Shen; Cristina L Zavaleta; Carsten H Nielsen; Christophe Mesangeau; Pradeep K Vuppala; Carmel Chan; Bonnie A Avery; James A Fishback; Rae R Matsumoto; Sanjiv S Gambhir; Christopher R McCurdy; Frederick T Chin
Journal:  J Med Chem       Date:  2012-09-20       Impact factor: 7.446

10.  Involvement of Chaperone Sigma1R in the Anxiolytic Effect of Fabomotizole.

Authors:  Mikhail V Voronin; Yulia V Vakhitova; Inna P Tsypysheva; Dmitry O Tsypyshev; Inna V Rybina; Rustam D Kurbanov; Elena V Abramova; Sergei B Seredenin
Journal:  Int J Mol Sci       Date:  2021-05-21       Impact factor: 5.923

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