Literature DB >> 25173703

Radioligand development for molecular imaging of the central nervous system with positron emission tomography.

Michael Honer1, Luca Gobbi1, Laurent Martarello1, Robert A Comley2.   

Abstract

Positron emission tomography (PET) is routinely used to support the development of drugs to treat neurological and psychiatric disorders. PET radioligands must not only be selective for the target of interest but must also possess a range of physicochemical and pharmacological characteristics that allow them to be radiolabelled with short-lived positron-emitting isotopes, safely administered to humans, and for the degree of target binding to be quantified in vivo. We review the ligand development process, including target selection, radioligand discovery (in vitro and preclinical evaluation), radiochemistry and evaluation in humans.
Copyright © 2014 Elsevier Ltd. All rights reserved.

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Year:  2014        PMID： 25173703     DOI： 10.1016/j.drudis.2014.08.012

Source DB:  PubMed          Journal:  Drug Discov Today        ISSN： 1359-6446            Impact factor:   7.851


  14 in total

Review 1.  (11)C[double bond, length as m-dash]O bonds made easily for positron emission tomography radiopharmaceuticals.

Authors:  Benjamin H Rotstein; Steven H Liang; Michael S Placzek; Jacob M Hooker; Antony D Gee; Frédéric Dollé; Alan A Wilson; Neil Vasdev
Journal:  Chem Soc Rev       Date:  2016-08-22       Impact factor: 54.564

2.  Performing radiosynthesis in microvolumes to maximize molar activity of tracers for positron emission tomography.

Authors:  Maxim E Sergeev; Mark Lazari; Federica Morgia; Jeffrey Collins; Muhammad Rashed Javed; Olga Sergeeva; Jason Jones; Michael E Phelps; Jason T Lee; Pei Yuin Keng; R Michael van Dam
Journal:  Commun Chem       Date:  2018-03-22

Review 3.  Tactics for preclinical validation of receptor-binding radiotracers.

Authors:  Susan Z Lever; Kuo-Hsien Fan; John R Lever
Journal:  Nucl Med Biol       Date:  2016-09-03       Impact factor: 2.408

4.  Synthesis and Characterization of Fluorine-18-Labeled N-(4-Chloro-3-((fluoromethyl-d2)thio)phenyl)picolinamide for Imaging of mGluR4 in Brain.

Authors:  Junfeng Wang; Xiying Qu; Timothy M Shoup; Gengyang Yuan; Sepideh Afshar; Chuzhi Pan; Aijun Zhu; Ji-Kyung Choi; Hye Jin Kang; Pekka Poutiainen; Georges El Fakhri; Zhaoda Zhang; Anna-Liisa Brownell
Journal:  J Med Chem       Date:  2020-03-04       Impact factor: 7.446

Review 5.  Mapping neuroreceptors with metal-labeled radiopharmaceuticals.

Authors:  S Chaturvedi; A Kaul; Puja P Hazari; Anil K Mishra
Journal:  Medchemcomm       Date:  2017-03-10       Impact factor: 3.597

6.  Single-Molecule Force Measurement Guides the Design of Multivalent Ligands with Picomolar Affinity.

Authors:  Zhen Yang; Sheng Jiang; Feng Li; Yatao Qiu; Jianhua Gu; Roderic I Pettigrew; Mauro Ferrari; Dale J Hamilton; Zheng Li
Journal:  Angew Chem Int Ed Engl       Date:  2019-02-18       Impact factor: 15.336

Review 7.  Update on PET Tracer Development for Muscarinic Acetylcholine Receptors.

Authors:  Marius Ozenil; Jonas Aronow; Marlon Millard; Thierry Langer; Wolfgang Wadsak; Marcus Hacker; Verena Pichler
Journal:  Pharmaceuticals (Basel)       Date:  2021-06-02

8.  In Vivo Imaging in Pharmaceutical Development and Its Impact on the 3Rs.

Authors:  Barry R Campbell; Dinko Gonzalez Trotter; Catherine D G Hines; Wenping Li; Manishkumar Patel; Weisheng Zhang; Jeffrey L Evelhoch
Journal:  ILAR J       Date:  2016-12

9.  Pharmacological agonists for more-targeted CNS radio-pharmaceuticals.

Authors:  Luc Zimmer
Journal:  Oncotarget       Date:  2016-12-06

Review 10.  Emerging PET Radiotracers and Targets for Imaging of Neuroinflammation in Neurodegenerative Diseases: Outlook Beyond TSPO.

Authors:  Vidya Narayanaswami; Kenneth Dahl; Vadim Bernard-Gauthier; Lee Josephson; Paul Cumming; Neil Vasdev
Journal:  Mol Imaging       Date:  2018 Jan-Dec       Impact factor: 4.488
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