Synthesis and preclinical evaluation of carbon-11 labelled N-((5-(4-fluoro-2-[C-11]methoxyphenyl) pyridin-3-yl) methyl) cyclopentanamine as a PET tracer for NR2B subunit-containing NMDA receptors

J.A.M. Christiaans; P.J. Klein; A. Metaxas; E.J.M. Kooijman; R.C. Schuit; J.E. Leysen; A.A. Lammertsma; B.N.M. van Berckel; A.D. Windhorst

doi:10.1016/j.nucmedbio.2014.04.131

Synthesis and preclinical evaluation of carbon-11 labelled N-((5-(4-fluoro-2-[C-11]methoxyphenyl) pyridin-3-yl) methyl) cyclopentanamine as a PET tracer for NR2B subunit-containing NMDA receptors

J.A.M. Christiaans, P.J. Klein, A. Metaxas, E.J.M. Kooijman, R.C. Schuit, J.E. Leysen, A.A. Lammertsma, B.N.M. van Berckel, A.D. Windhorst

Research output: Contribution to Journal › Article › Academic › peer-review

Abstract

Introduction: The N-methyl-D-Aspartate (NMDA) receptor plays an important role in learning and memory. Overactivation is thought to play an important role in neurodegenerative disorders such as Alzheimer's disease. Currently, it is not possible to assess N-methyl-D-aspartate receptor (NMDAr) bio-availability in vivo. The purpose of this study was to develop a positron emission tomography (PET) ligand for the NR2B binding site of the NMDA receptor. Methods: N-((5-(4-fluoro-2-methoxyphenyl)pyridin-3-yl)methyl)cyclopentanamine was radiolabelled with carbon-11 in the phenyl moiety. Biodistribution and blocking studies were carried out in anaesthetized mice and in non-anaesthetized rats. Results: N-((5-(4-fluoro-2-[

Original language	English
Pages (from-to)	670-680
Journal	Nuclear Medicine and Biology
Volume	41
Issue number	8
DOIs	https://doi.org/10.1016/j.nucmedbio.2014.04.131
Publication status	Published - 2014

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Christiaans, J. A. M., Klein, P. J., Metaxas, A., Kooijman, E. J. M., Schuit, R. C., Leysen, J. E., Lammertsma, A. A., van Berckel, B. N. M., & Windhorst, A. D. (2014). Synthesis and preclinical evaluation of carbon-11 labelled N-((5-(4-fluoro-2-[C-11]methoxyphenyl) pyridin-3-yl) methyl) cyclopentanamine as a PET tracer for NR2B subunit-containing NMDA receptors. Nuclear Medicine and Biology, 41(8), 670-680. https://doi.org/10.1016/j.nucmedbio.2014.04.131

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title = "Synthesis and preclinical evaluation of carbon-11 labelled N-((5-(4-fluoro-2-[C-11]methoxyphenyl) pyridin-3-yl) methyl) cyclopentanamine as a PET tracer for NR2B subunit-containing NMDA receptors",

abstract = "Introduction: The N-methyl-D-Aspartate (NMDA) receptor plays an important role in learning and memory. Overactivation is thought to play an important role in neurodegenerative disorders such as Alzheimer's disease. Currently, it is not possible to assess N-methyl-D-aspartate receptor (NMDAr) bio-availability in vivo. The purpose of this study was to develop a positron emission tomography (PET) ligand for the NR2B binding site of the NMDA receptor. Methods: N-((5-(4-fluoro-2-methoxyphenyl)pyridin-3-yl)methyl)cyclopentanamine was radiolabelled with carbon-11 in the phenyl moiety. Biodistribution and blocking studies were carried out in anaesthetized mice and in non-anaesthetized rats. Results: N-((5-(4-fluoro-2-[",

author = "J.A.M. Christiaans and P.J. Klein and A. Metaxas and E.J.M. Kooijman and R.C. Schuit and J.E. Leysen and A.A. Lammertsma and {van Berckel}, B.N.M. and A.D. Windhorst",

year = "2014",

doi = "10.1016/j.nucmedbio.2014.04.131",

language = "English",

volume = "41",

pages = "670--680",

journal = "Nuclear Medicine and Biology",

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Christiaans, JAM, Klein, PJ, Metaxas, A, Kooijman, EJM, Schuit, RC, Leysen, JE, Lammertsma, AA, van Berckel, BNM & Windhorst, AD 2014, 'Synthesis and preclinical evaluation of carbon-11 labelled N-((5-(4-fluoro-2-[C-11]methoxyphenyl) pyridin-3-yl) methyl) cyclopentanamine as a PET tracer for NR2B subunit-containing NMDA receptors', Nuclear Medicine and Biology, vol. 41, no. 8, pp. 670-680. https://doi.org/10.1016/j.nucmedbio.2014.04.131

Synthesis and preclinical evaluation of carbon-11 labelled N-((5-(4-fluoro-2-[C-11]methoxyphenyl) pyridin-3-yl) methyl) cyclopentanamine as a PET tracer for NR2B subunit-containing NMDA receptors. / Christiaans, J.A.M.; Klein, P.J.; Metaxas, A. et al.
In: Nuclear Medicine and Biology, Vol. 41, No. 8, 2014, p. 670-680.

Research output: Contribution to Journal › Article › Academic › peer-review

TY - JOUR

T1 - Synthesis and preclinical evaluation of carbon-11 labelled N-((5-(4-fluoro-2-[C-11]methoxyphenyl) pyridin-3-yl) methyl) cyclopentanamine as a PET tracer for NR2B subunit-containing NMDA receptors

AU - Christiaans, J.A.M.

AU - Klein, P.J.

AU - Metaxas, A.

AU - Kooijman, E.J.M.

AU - Schuit, R.C.

AU - Leysen, J.E.

AU - Lammertsma, A.A.

AU - van Berckel, B.N.M.

AU - Windhorst, A.D.

PY - 2014

Y1 - 2014

N2 - Introduction: The N-methyl-D-Aspartate (NMDA) receptor plays an important role in learning and memory. Overactivation is thought to play an important role in neurodegenerative disorders such as Alzheimer's disease. Currently, it is not possible to assess N-methyl-D-aspartate receptor (NMDAr) bio-availability in vivo. The purpose of this study was to develop a positron emission tomography (PET) ligand for the NR2B binding site of the NMDA receptor. Methods: N-((5-(4-fluoro-2-methoxyphenyl)pyridin-3-yl)methyl)cyclopentanamine was radiolabelled with carbon-11 in the phenyl moiety. Biodistribution and blocking studies were carried out in anaesthetized mice and in non-anaesthetized rats. Results: N-((5-(4-fluoro-2-[

AB - Introduction: The N-methyl-D-Aspartate (NMDA) receptor plays an important role in learning and memory. Overactivation is thought to play an important role in neurodegenerative disorders such as Alzheimer's disease. Currently, it is not possible to assess N-methyl-D-aspartate receptor (NMDAr) bio-availability in vivo. The purpose of this study was to develop a positron emission tomography (PET) ligand for the NR2B binding site of the NMDA receptor. Methods: N-((5-(4-fluoro-2-methoxyphenyl)pyridin-3-yl)methyl)cyclopentanamine was radiolabelled with carbon-11 in the phenyl moiety. Biodistribution and blocking studies were carried out in anaesthetized mice and in non-anaesthetized rats. Results: N-((5-(4-fluoro-2-[

U2 - 10.1016/j.nucmedbio.2014.04.131

DO - 10.1016/j.nucmedbio.2014.04.131

M3 - Article

SN - 0969-8051

VL - 41

SP - 670

EP - 680

JO - Nuclear Medicine and Biology

JF - Nuclear Medicine and Biology

IS - 8

ER -

Synthesis and preclinical evaluation of carbon-11 labelled N-((5-(4-fluoro-2-[C-11]methoxyphenyl) pyridin-3-yl) methyl) cyclopentanamine as a PET tracer for NR2B subunit-containing NMDA receptors

Abstract

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