Synthesis and Characterization in Rodent Brain of the Subtype-Selective NR2B NMDA Receptor Ligand [11C]Ro04-5595 as a Potential Radiotracer for Positron Emission Tomography | Zendy

Jimmy E. Jakobsson | Zendy; Eleni Gourni | Zendy; Shivashankar Khanapur | Zendy; Beatriz Brito | Zendy; Patrick J. Riss | Zendy

Open Access

Synthesis and Characterization in Rodent Brain of the Subtype-Selective NR2B NMDA Receptor Ligand [¹¹C]Ro04-5595 as a Potential Radiotracer for Positron Emission Tomography

Author(s) -

Jimmy E. Jakobsson,

Eleni Gourni,

Shivashankar Khanapur,

Beatriz Brito,

Patrick J. Riss

Publication year - 2019

Publication title -

acs omega

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.779

H-Index - 40

ISSN - 2470-1343

DOI - 10.1021/acsomega.9b00357

Subject(s) - nmda receptor , radioligand , positron emission tomography , in vivo , ligand (biochemistry) , chemistry , receptor , pet imaging , preclinical imaging , protein subunit , biophysics , nuclear medicine , biochemistry , biology , medicine , microbiology and biotechnology , gene

The NR2B subunit of the N -methyl-d-aspartate (NMDA) receptor has been implicated in controlling synaptic plasticity, memory, and learning. Herein, we describe an 11 C-labeled PET radiotracer based on 1-(4-chlorophenethyl)-6-methoxy-2-methyl-1,2,3,4-tetrahydroisoquinolin-7-ol, Ro04-5595. The radiotracer was evaluated in rats using PET. The PET study showed a good pharmacokinetic profile with rapid uptake and washout over 90 min. Complementary high-resolution autoradiographic images using [ 3 H]Ro04-5595 demonstrated strong binding in NR2B receptor-rich regions and low binding in cerebellum where NR2B concentration is low. We conclude to have developed a selective NR2B receptor radioligand suitable for quantitative and qualitative imaging of a NR2B receptor distribution in vitro and in vivo.

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