Evidence map›Paper›PMID 30145376›Full record

ArticleEuropean journal of medicinal chemistry2018

Synthesis, pharmacology and preclinical evaluation of

Zhen Chen, Wakana Mori, Xiaofei Zhang, Tomoteru Yamasaki, Patrick J Dunn, Genwei Zhang, Hualong Fu, Tuo Shao, Yiding Zhang, Akiko Hatori and 13 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in European journal of medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.

0numbers the graph read from it
0cells of the map it votes in
14citing papers in PubMed
1.3field-weighted citation impact, top 23% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

14 citing papers in PubMed, 22 citations in OpenAlex.

  1. Preclinical Evaluation of [Molecular imaging and biology · 2026
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  9. Review
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  11. Development of a highly-specificActa pharmaceutica Sinica. B · 2021
    Article
  12. Synthesis and evaluation of 6-(Bioorganic & medicinal chemistry letters · 2020
    Article
  13. Article
  14. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

23 authors at 5 institutions in 3 countries.

Zhen ChenDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Boston, MA, 02114, USA; Department of Chemistry, School of Science, Tianjin University, 92 Weijin Road, Nankai District, Tianjin 300072, China.
Wakana MoriDepartment of Radiopharmaceutics Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Chiba, 263-8555, Japan.
Xiaofei ZhangDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Boston, MA, 02114, USA.
Tomoteru YamasakiDepartment of Radiopharmaceutics Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Chiba, 263-8555, Japan.
Patrick J DunnDepartment of Cellular and Molecular Physiology, Department of Neuroscience, Yale University School of Medicine, New Haven, CT, USA.
Genwei ZhangDepartment of Chemistry and Biochemistry, University of Oklahoma, Norman, OK, 73019, USA.
Hualong FuDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Boston, MA, 02114, USA.
Tuo ShaoDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Boston, MA, 02114, USA.
Yiding ZhangDepartment of Radiopharmaceutics Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Chiba, 263-8555, Japan.
Akiko HatoriDepartment of Radiopharmaceutics Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Chiba, 263-8555, Japan.
Longle MaDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Boston, MA, 02114, USA.
Masayuki FujinagaDepartment of Radiopharmaceutics Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Chiba, 263-8555, Japan.
Lin XieDepartment of Radiopharmaceutics Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Chiba, 263-8555, Japan.
Xiaoyun DengDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Boston, MA, 02114, USA.
Hua LiDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Boston, MA, 02114, USA.
Qingzhen YuDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Boston, MA, 02114, USA.
Jian RongDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Boston, MA, 02114, USA.
Lee JosephsonDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Boston, MA, 02114, USA.
Jun-An MaDepartment of Chemistry, School of Science, Tianjin University, 92 Weijin Road, Nankai District, Tianjin 300072, China.
Yihan ShaoDepartment of Chemistry and Biochemistry, University of Oklahoma, Norman, OK, 73019, USA.
Susumu TomitaDepartment of Cellular and Molecular Physiology, Department of Neuroscience, Yale University School of Medicine, New Haven, CT, USA.
Ming-Rong ZhangDepartment of Radiopharmaceutics Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Chiba, 263-8555, Japan. Electronic address: zhang.ming-rong@qst.go.jp.
Steven H LiangDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Boston, MA, 02114, USA. Electronic address: liang.steven@mgh.harvard.edu.
Harvard University · USNational Institutes for Quantum Science and Technology · JPUniversity of Oklahoma · USYale University · USTianjin University · CN

Funding

Translational CoreP01DK057751 · NIDDK · YALE UNIVERSITY · PI MITCHELL, KISHA A · 2001 to 2020
$25.6M
INSTITUTIONAL NATIONAL RESEARCH SERVICE AWARDT32GM007324 · NIGMS · YALE UNIVERSITY · PI BENNETT, ANTON M · 1987 to 2022
$6.2M
Regulation of glutamate receptors by calcium-dependent protein kinasesR01MH077939 · NIMH · YALE UNIVERSITY · PI TOMITA, SUSUMU · 2008 to 2023
$5.2M
In vivo Probe for ionotropic glutamate signaling system: AMPA receptorsR01MH120197 · NIMH · MASSACHUSETTS GENERAL HOSPITAL · PI LIANG, STEVEN H · 2019 to 2021
$2.4M
Neuro-PET Radiotracer Discovery for Imaging Glycogen Synthase Kinase-3R01AG054473 · NIA · MASSACHUSETTS GENERAL HOSPITAL · PI VASDEV, NEIL · 2017 to 2020
$1.7M
PET ligand development for mGlu2 based on negative allosteric modulatorsR01MH117125 · NIMH · MASSACHUSETTS GENERAL HOSPITAL · PI LIANG, STEVEN H · 2018 to 2020
$1.6M
New PET tracers for neuroimaging of FAAH in endocannabinoid signalingK01DA038000 · NIDA · MASSACHUSETTS GENERAL HOSPITAL · PI LIANG, STEVEN H · 2014 to 2018
$927k
Novel PET Tracers for Imaging Monoacylglycerol Lipase in Endocannabinoid SignalingR33DA043507 · NIDA · MASSACHUSETTS GENERAL HOSPITAL · PI LIANG, STEVEN H · 2019 to 2021
$851k
Novel PET Tracers for Imaging Monoacylglycerol Lipase in Endocannabinoid SignalingR21DA043507 · NIDA · MASSACHUSETTS GENERAL HOSPITAL · PI LIANG, STEVEN H · 2017 to 2018
$425k
NIA NIH HHS R01 AG054473NIDA NIH HHS K01 DA038000NIDA NIH HHS R21 DA043507NIDA NIH HHS R33 DA043507NIDDK NIH HHS P01 DK057751NIGMS NIH HHS T32 GM007324NIMH NIH HHS R01 MH077939NIMH NIH HHS R01 MH117125NIMH NIH HHS R01 MH120197
6 · The paper itself

Abstract

a-Amino-3-hydroxyl-5-methyl-4-isoxazolepropionic acid (AMPA) receptors are implicated in the pathology of neurological diseases such as epilepsy and schizophrenia. As pan antagonists for this target are often accompanied with undesired effects at high doses, one of the recent drug discovery approaches has shifted to subtype-selective AMPA receptor (AMPAR) antagonists, specifically, via modulating transmembrane AMPAR regulatory proteins (TARPs). The quantification of AMPARs by positron emission tomography (PET) would help obtain insights into disease conditions in the living brain and advance the translational development of AMPAR antagonists. Herein we report the design, synthesis and preclinical evaluation of a series of TARP γ-8 antagonists, amenable for radiolabeling, for the development of subtype-selective AMPAR PET imaging agents. Based on the pharmacology evaluation, molecular docking studies and physiochemical properties, we have identified several promising lead compounds 3, 17-19 and 21 for in vivo PET studies. All candidate compounds were labeled with [

Indexed as

Carbon RadioisotopesDose-Response Relationship, DrugHumansImidazolesMolecular ImagingMolecular ProbesMolecular StructurePositron-Emission TomographyReceptors, AMPAStructure-Activity Relationship1,3-dihydro-2H-benzo(d)imidazole-2-oneCarbon RadioisotopesImidazolesMolecular ProbesReceptors, AMPAAMPAEpilepsyIonotropic glutamate receptorPositron emission tomographyTARPTransmembrane AMPA receptor regulatory protein

Identifiers

PMID30145376
PMCPMC6245653
OpenAlexW2887971671

What OpenQuestion holds

Textmetadata
LicenceTDM
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.