Literature DB >> 11056369

Synthesis and binding characteristics of N-(1-naphthyl)-N'-(3-[(125)I]-iodophenyl)-N'-methylguanidine ([(125)I]-CNS 1261): a potential SPECT agent for imaging NMDA receptor activation.

J Owens1, A A Tebbutt, A L McGregor, K Kodama, S S Magar, M E Perlman, D J Robins, G J Durant, J McCulloch.   

Abstract

N-(1-Naphthyl)-N'-(3-[(125)I]-iodophenyl)-N'-methylguanidine ([(125)I]-CNS 1261) was synthesized as a potential radioligand to image N-methyl-D-aspartate (NMDA) receptor activation. [(125)I]-CNS 1261 was prepared by radioiodination of N-(1-naphthyl)-N'-(3-tributylstannylphenyl)-N'-methylguanidine using Na(125)I and peracetic acid. [(125)I]-CNS 1261 uptake in vivo reflected NMDA receptor distribution in normal rat brain, whereas in ischemic rat brain, uptake was markedly increased in areas of NMDA receptor activation. Radiolabeled CNS 1261 appears to be a good candidate for further development as a single photon emission computed tomography tracer in the investigation of NMDA receptor activation in cerebral ischemia.

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Year:  2000        PMID： 11056369     DOI： 10.1016/s0969-8051(00)00102-5

Source DB:  PubMed          Journal:  Nucl Med Biol        ISSN： 0969-8051            Impact factor:   2.408


  11 in total

1.  Quantification of recombinant and platelet P2Y(1) receptors utilizing a [(125)I]-labeled high-affinity antagonist 2-iodo-N(6)-methyl-(N)-methanocarba-2'-deoxyadenosine-3',5'-bisphosphate ([(125)I]MRS2500).

Authors:  Philippe Ohlmann; Sonia de Castro; Garth G Brown; Christian Gachet; Kenneth A Jacobson; T Kendall Harden
Journal:  Pharmacol Res       Date:  2010-06-04       Impact factor: 7.658

2.  Development of Radiolabeled Ligands Targeting the Glutamate Binding Site of the N-Methyl-d-aspartate Receptor as Potential Imaging Agents for Brain.

Authors:  Lucia Tamborini; Ying Chen; Catherine A Foss; Andrea Pinto; Andrew G Horti; Stephen F Traynelis; Carlo De Micheli; Ronnie C Mease; Kasper B Hansen; Paola Conti; Martin G Pomper
Journal:  J Med Chem       Date:  2016-12-06       Impact factor: 7.446

Review 3.  Positron Emission Tomography (PET) Ligand Development for Ionotropic Glutamate Receptors: Challenges and Opportunities for Radiotracer Targeting N-Methyl-d-aspartate (NMDA), α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA), and Kainate Receptors.

Authors:  Hualong Fu; Zhen Chen; Lee Josephson; Zijing Li; Steven H Liang
Journal:  J Med Chem       Date:  2018-08-27       Impact factor: 7.446

4.  New N-aryl-N'-(3-(substituted)phenyl)-N'-methylguanidines as leads to potential PET radioligands for imaging the open NMDA receptor.

Authors:  Gregory R Naumiec; Lisheng Cai; Victor W Pike
Journal:  Bioorg Med Chem Lett       Date:  2014-11-29       Impact factor: 2.823

Review 5.  Selected PET Radioligands for Ion Channel Linked Neuroreceptor Imaging: Focus on GABA, NMDA and nACh Receptors.

Authors:  Alina Kassenbrock; Neil Vasdev; Steven H Liang
Journal:  Curr Top Med Chem       Date:  2016       Impact factor: 3.295

6.  Relationship between ketamine-induced psychotic symptoms and NMDA receptor occupancy: a [(123)I]CNS-1261 SPET study.

Authors:  James M Stone; Kjell Erlandsson; Erik Arstad; Lisa Squassante; Vincenzo Teneggi; Rodrigo A Bressan; John H Krystal; Peter J Ell; Lyn S Pilowsky
Journal:  Psychopharmacology (Berl)       Date:  2008-01-05       Impact factor: 4.530

7.  Dynamic changes in N-methyl-D-aspartate receptors after closed head injury in mice: Implications for treatment of neurological and cognitive deficits.

Authors:  Anat Biegon; Pamela A Fry; Charles M Paden; Alexander Alexandrovich; Jeanna Tsenter; Esther Shohami
Journal:  Proc Natl Acad Sci U S A       Date:  2004-03-24       Impact factor: 11.205

8.  N'-3-(Trifluoromethyl)phenyl Derivatives of N-Aryl-N'-methylguanidines as Prospective PET Radioligands for the Open Channel of the N-Methyl-d-aspartate (NMDA) Receptor: Synthesis and Structure-Affinity Relationships.

Authors:  Gregory R Naumiec; Kimberley J Jenko; Sami S Zoghbi; Robert B Innis; Lisheng Cai; Victor W Pike
Journal:  J Med Chem       Date:  2015-12-04       Impact factor: 7.446

Review 9.  Development of PET and SPECT probes for glutamate receptors.

Authors:  Takeshi Fuchigami; Morio Nakayama; Sakura Yoshida
Journal:  ScientificWorldJournal       Date:  2015-03-22

Review 10.  Design of Radioiodinated Pharmaceuticals: Structural Features Affecting Metabolic Stability towards in Vivo Deiodination.

Authors:  Lorenzo Cavina; Dion van der Born; Peter H M Klaren; Martin C Feiters; Otto C Boerman; Floris P J T Rutjes
Journal:  European J Org Chem       Date:  2017-04-26
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