Literature DB >> 24446373

Discovery of heterocyclic nonacetamide synaptic vesicle protein 2A (SV2A) ligands with single-digit nanomolar potency: opening avenues towards the first SV2A positron emission tomography (PET) ligands.

Joël Mercier1, Laurence Archen, Véronique Bollu, Stéphane Carré, Yves Evrard, Eric Jnoff, Benoît Kenda, Bénédicte Lallemand, Philippe Michel, Florian Montel, Florence Moureau, Nathalie Price, Yannick Quesnel, Xavier Sauvage, Anne Valade, Laurent Provins.   

Abstract

The role of the synaptic vesicle protein 2A (SV2A) protein, target of the antiepileptic drug levetiracetam, is still mostly unknown. Considering its potential to provide in vivo functional insights into the role of SV2A in epileptic patients, the development of an SV2A positron emission tomography (PET) tracer has been undertaken. Using a 3D pharmacophore model based on close analogues of levetiracetam, we report the rationale design of three heterocyclic non-acetamide lead compounds, UCB-A, UCB-H and UCB-J, the first single-digit nanomolar SV2A ligands with suitable properties for development as PET tracers.
© 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Entities:  

Keywords:  epilepsy; imaging agents; levetiracetam; positron emission tomography (PET); synaptic vesicle proteins; tracers

Mesh：

Substances：

Year:  2014        PMID： 24446373     DOI： 10.1002/cmdc.201300482

Source DB:  PubMed          Journal:  ChemMedChem        ISSN： 1860-7179            Impact factor:   3.466


  21 in total

1.  Synthesis and in Vivo Evaluation of a Novel PET Radiotracer for Imaging of Synaptic Vesicle Glycoprotein 2A (SV2A) in Nonhuman Primates.

Authors:  Songye Li; Zhengxin Cai; Xiaoai Wu; Daniel Holden; Richard Pracitto; Michael Kapinos; Hong Gao; David Labaree; Nabeel Nabulsi; Richard E Carson; Yiyun Huang
Journal:  ACS Chem Neurosci       Date:  2018-11-16       Impact factor: 4.418

2.  Synthesis and in vivo evaluation of [18F]UCB-J for PET imaging of synaptic vesicle glycoprotein 2A (SV2A).

Authors:  Songye Li; Zhengxin Cai; Wenjie Zhang; Daniel Holden; Shu-Fei Lin; Sjoerd J Finnema; Anupama Shirali; Jim Ropchan; Stephane Carre; Joel Mercier; Richard E Carson; Nabeel Nabulsi; Yiyun Huang
Journal:  Eur J Nucl Med Mol Imaging       Date:  2019-06-07       Impact factor: 9.236

3.  Prolonged anesthesia alters brain synaptic architecture.

Authors:  Michael Wenzel; Alexander Leunig; Shuting Han; Darcy S Peterka; Rafael Yuste
Journal:  Proc Natl Acad Sci U S A       Date:  2021-02-16       Impact factor: 11.205

4.  Radiosynthesis of (11)C-Levetiracetam: A Potential Marker for PET Imaging of SV2A Expression.

Authors:  Hancheng Cai; Thomas J Mangner; Otto Muzik; Ming-Wei Wang; Diane C Chugani; Harry T Chugani
Journal:  ACS Med Chem Lett       Date:  2014-08-19       Impact factor: 4.345

5.  Lower prefrontal cortical synaptic vesicle binding in cocaine use disorder: An exploratory 11 C-UCB-J positron emission tomography study in humans.

Authors:  Gustavo A Angarita; Patrick D Worhunsky; Mika Naganawa; Takuya Toyonaga; Nabeel B Nabulsi; Chiang-Shan R Li; Irina Esterlis; Patrick D Skosnik; Rajiv Radhakrishnan; Brian Pittman; Ralitza Gueorguieva; Marc N Potenza; Sjoerd J Finnema; Yiyun Huang; Richard E Carson; Robert T Malison
Journal:  Addict Biol       Date:  2021-12-01       Impact factor: 4.280

Review 6.  Using molecular imaging to understand early schizophrenia-related psychosis neurochemistry: a review of human studies.

Authors:  Christin Schifani; Sina Hafizi; Tania Da Silva; Jeremy Joseph Watts; M Saad Khan; Romina Mizrahi
Journal:  Int Rev Psychiatry       Date:  2017-12-08

Review 7.  PET imaging of synaptic density: A new tool for investigation of neuropsychiatric diseases.

Authors:  Zhengxin Cai; Songye Li; David Matuskey; Nabeel Nabulsi; Yiyun Huang
Journal:  Neurosci Lett       Date:  2018-07-31       Impact factor: 3.046

8.  In vivo imaging of synaptic SV2A protein density in healthy and striatal-lesioned rats with [11C]UCB-J PET.

Authors:  Majken B Thomsen; Jan Jacobsen; Thea P Lillethorup; Anna C Schacht; Mette Simonsen; Marina Romero-Ramos; David J Brooks; Anne M Landau
Journal:  J Cereb Blood Flow Metab       Date:  2020-06-14       Impact factor: 6.200

9.  Kinetics and 28-day test-retest repeatability and reproducibility of [11C]UCB-J PET brain imaging.

Authors:  Hayel Tuncel; Ronald Boellaard; Emma M Coomans; Erik Fj de Vries; Andor Wjm Glaudemans; Paula Kopschina Feltes; David V García; Sander Cj Verfaillie; Emma E Wolters; Steven P Sweeney; J Michael Ryan; Magnus Ivarsson; Berkley A Lynch; Patrick Schober; Philip Scheltens; Robert C Schuit; Albert D Windhorst; Peter P De Deyn; Bart Nm van Berckel; Sandeep Sv Golla
Journal:  J Cereb Blood Flow Metab       Date:  2020-10-08       Impact factor: 6.200

10.  Quantification of SV2A Binding in Rodent Brain Using [18F]SynVesT-1 and PET Imaging.

Authors:  Pragalath Sadasivam; Xiaotian T Fang; Takuya Toyonaga; Supum Lee; Yuping Xu; Ming-Qiang Zheng; Joshua Spurrier; Yiyun Huang; Stephen M Strittmatter; Richard E Carson; Zhengxin Cai
Journal:  Mol Imaging Biol       Date:  2020-11-30       Impact factor: 3.484
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.