Literature DB >> 27087244

Considerations in the Development of Reversibly Binding PET Radioligands for Brain Imaging.

Victor W Pike1.   

Abstract

The development of reversibly binding radioligands for imaging brain proteins in vivo, such as enzymes, neurotransmitter transporters, receptors and ion channels, with positron emission tomography (PET) is keenly sought for biomedical studies of neuropsychiatric disorders and for drug discovery and development, but is recognized as being highly challenging at the medicinal chemistry level. This article aims to compile and discuss the main considerations to be taken into account by chemists embarking on programs of radioligand development for PET imaging of brain protein targets.

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Year:  2016        PMID： 27087244      PMCID： PMC5579844          DOI： 10.2174/0929867323666160418114826

Source DB:  PubMed          Journal:  Curr Med Chem        ISSN： 0929-8673            Impact factor:   4.530


  330 in total

1.  Rapid calculation of polar molecular surface area and its application to the prediction of transport phenomena. 2. Prediction of blood-brain barrier penetration.

Authors:  D E Clark
Journal:  J Pharm Sci       Date:  1999-08       Impact factor: 3.534

2.  Cu(I)-mediated (18)F-trifluoromethylation of arenes: rapid synthesis of (18)F-labeled trifluoromethyl arenes.

Authors:  T Rühl; W Rafique; V T Lien; P J Riss
Journal:  Chem Commun (Camb)       Date:  2014-04-28       Impact factor: 6.222

3.  First-in-human PET quantification study of cerebral α4β2* nicotinic acetylcholine receptors using the novel specific radioligand (-)-[(18)F]Flubatine.

Authors:  Osama Sabri; Georg-Alexander Becker; Philipp M Meyer; Swen Hesse; Stephan Wilke; Susanne Graef; Marianne Patt; Julia Luthardt; Gudrun Wagenknecht; Alexander Hoepping; René Smits; Annegret Franke; Bernhard Sattler; Bernd Habermann; Petra Neuhaus; Steffen Fischer; Solveig Tiepolt; Winnie Deuther-Conrad; Henryk Barthel; Peter Schönknecht; Peter Brust
Journal:  Neuroimage       Date:  2015-05-30       Impact factor: 6.556

4.  Quantitative PET analyses of regional [11C]PE2I binding to the dopamine transporter--application to juvenile myoclonic epilepsy.

Authors:  Ikuo Odano; Andrea Varrone; Ivanka Savic; Carolina Ciumas; Per Karlsson; Aurelija Jucaite; Christer Halldin; Lars Farde
Journal:  Neuroimage       Date:  2011-10-28       Impact factor: 6.556

5.  Evaluation of ultrafiltration for the free-fraction determination of single photon emission computed tomography (SPECT) radiotracers: beta-CIT, IBF, and iomazenil.

Authors:  M S Gandelman; R M Baldwin; S S Zoghbi; Y Zea-Ponce; R B Innis
Journal:  J Pharm Sci       Date:  1994-07       Impact factor: 3.534

6.  Routine production of [(18)f]flumazenil from iodonium tosylate using a sample pretreatment method: a 2.5-year production report.

Authors:  Byung Seok Moon; Jun Hyung Park; Hong Jin Lee; Byung Chul Lee; Sang Eun Kim
Journal:  Mol Imaging Biol       Date:  2014-10       Impact factor: 3.488

7.  [3H]WAY-100635 for 5-HT1A receptor autoradiography in human brain: a comparison with [3H]8-OH-DPAT and demonstration of increased binding in the frontal cortex in schizophrenia.

Authors:  P W Burnet; S L Eastwood; P J Harrison
Journal:  Neurochem Int       Date:  1997-06       Impact factor: 3.921

8.  Species differences in mGluR5 binding sites in mammalian central nervous system determined using in vitro binding with [18F]F-PEB.

Authors:  Shil Patel; Terence G Hamill; Brett Connolly; Elaine Jagoda; Wenping Li; Raymond E Gibson
Journal:  Nucl Med Biol       Date:  2007-09-19       Impact factor: 2.408

Review 9.  11CO2 fixation: a renaissance in PET radiochemistry.

Authors:  Benjamin H Rotstein; Steven H Liang; Jason P Holland; Thomas Lee Collier; Jacob M Hooker; Alan A Wilson; Neil Vasdev
Journal:  Chem Commun (Camb)       Date:  2013-05-14       Impact factor: 6.222

10.  Improved synthesis of some commonly used PET radioligands by the use of [11C]methyl triflate.

Authors:  K Någren; L Müller; C Halldin; C G Swahn; P Lehikoinen
Journal:  Nucl Med Biol       Date:  1995-02       Impact factor: 2.408
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  67 in total

1.  Design, synthesis and evaluation of 111In labeled DOTA-conjugated tetrapeptides having high affinity and selectivity for mu opioid receptors.

Authors:  John R Lever; Emily A Fergason-Cantrell; Terry L Carmack; Lisa D Watkinson; Fabio Gallazzi
Journal:  Nucl Med Biol       Date:  2019-03-07       Impact factor: 2.408

2.  Synthesis and Preliminary Evaluation of [11 C]GNE-1023 as a Potent PET Probe for Imaging Leucine-Rich Repeat Kinase 2 (LRRK2) in Parkinson's Disease.

Authors:  Zhen Chen; Tuo Shao; Wei Gao; Hualong Fu; Thomas Lee Collier; Jian Rong; Xiaoyun Deng; Qingzhen Yu; Xiaofei Zhang; April T Davenport; James B Daunais; Hsiao-Ying Wey; Yihan Shao; Lee Josephson; Wen-Wei Qiu; Steven Liang
Journal:  ChemMedChem       Date:  2019-08-22       Impact factor: 3.466

3.  3-Substituted 1,5-Diaryl-1 H-1,2,4-triazoles as Prospective PET Radioligands for Imaging Brain COX-1 in Monkey. Part 2: Selection and Evaluation of [11C]PS13 for Quantitative Imaging.

Authors:  Stal Shrestha; Prachi Singh; Michelle Y Cortes-Salva; Kimberly J Jenko; Masamichi Ikawa; Min-Jeong Kim; Masato Kobayashi; Cheryl L Morse; Robert L Gladding; Jeih-San Liow; Sami S Zoghbi; Masahiro Fujita; Robert B Innis; Victor W Pike
Journal:  ACS Chem Neurosci       Date:  2018-06-13       Impact factor: 4.418

4.  Synthesis and Preliminary Evaluations of a Triazole-Cored Antagonist as a PET Imaging Probe ([18F]N2B-0518) for GluN2B Subunit in the Brain.

Authors:  Hualong Fu; Weiting Tang; Zhen Chen; Vasily V Belov; Genwei Zhang; Tuo Shao; Xiaofei Zhang; Qingzhen Yu; Jian Rong; Xiaoyun Deng; Wei Han; Scott J Myers; Pilar Giffenig; Lu Wang; Lee Josephson; Yihan Shao; April T Davenport; James B Daunais; Mikhail Papisov; Hongjie Yuan; Zijing Li; Stephen F Traynelis; Steven H Liang
Journal:  ACS Chem Neurosci       Date:  2019-02-27       Impact factor: 4.418

5.  Potent and Selective Tetrahydroisoquinoline Kappa Opioid Receptor Antagonists of Lead Compound (3 R)- N-[1 R)-1-(Cyclohexylmethyl)-2-methylpropyl]-7-hydroxy-1,2,3,4-tetrahydroisoquinoline-3-carboxamide (CDTic).

Authors:  Chad M Kormos; Pauline W Ondachi; Scott P Runyon; James B Thomas; S Wayne Mascarella; Ann M Decker; Hernán A Navarro; Timothy R Fennell; Rodney W Snyder; F Ivy Carroll
Journal:  J Med Chem       Date:  2018-08-29       Impact factor: 7.446

6.  [11 C]Fluoroform, a Breakthrough for Versatile Labeling of PET Radiotracer Trifluoromethyl Groups in High Molar Activity.

Authors:  Mohammad B Haskali; Victor W Pike
Journal:  Chemistry       Date:  2017-05-17       Impact factor: 5.236

Review 7.  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

8.  Synthesis and Preliminary Studies of a Novel Negative Allosteric Modulator, 7-((2,5-Dioxopyrrolidin-1-yl)methyl)-4-(2-fluoro-4-[11C]methoxyphenyl) quinoline-2-carboxamide, for Imaging of Metabotropic Glutamate Receptor 2.

Authors:  Xiaofei Zhang; Katsushi Kumata; Tomoteru Yamasaki; Ran Cheng; Akiko Hatori; Longle Ma; Yiding Zhang; Lin Xie; Lu Wang; Hye Jin Kang; Douglas J Sheffler; Nicholas D P Cosford; Ming-Rong Zhang; Steven H Liang
Journal:  ACS Chem Neurosci       Date:  2017-06-13       Impact factor: 4.418

9.  Synthesis, pharmacology and preclinical evaluation of 11C-labeled 1,3-dihydro-2H-benzo[d]imidazole-2-ones for imaging γ8-dependent transmembrane AMPA receptor regulatory protein.

Authors:  Zhen Chen; Wakana Mori; Xiaofei Zhang; Tomoteru Yamasaki; Patrick J Dunn; Genwei Zhang; Hualong Fu; Tuo Shao; Yiding Zhang; Akiko Hatori; Longle Ma; Masayuki Fujinaga; Lin Xie; Xiaoyun Deng; Hua Li; Qingzhen Yu; Jian Rong; Lee Josephson; Jun-An Ma; Yihan Shao; Susumu Tomita; Ming-Rong Zhang; Steven H Liang
Journal:  Eur J Med Chem       Date:  2018-08-09       Impact factor: 6.514

10.  Translocator protein ligands based on N-methyl-(quinolin-4-yl)oxypropanamides with properties suitable for PET radioligand development.

Authors:  Chad Brouwer; Kimberly J Jenko; Sami S Zoghbi; Cheryl L Morse; Robert B Innis; Victor W Pike
Journal:  Eur J Med Chem       Date:  2016-08-25       Impact factor: 6.514
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