Synthesis, structure activity relationship, radiolabeling and preclinical evaluation of high affinity ligands for the ion channel of the N-methyl-D-aspartate receptor as potential imaging probes for positron emission tomography

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

doi:10.1016/j.bmc.2014.12.029

Synthesis, structure activity relationship, radiolabeling and preclinical evaluation of high affinity ligands for the ion channel of the N-methyl-D-aspartate receptor as potential imaging probes for positron emission tomography

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

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

Abstract

The N-methyl-d-aspartate receptor (NMDAr) is involved in many neurological and psychiatric disorders including Alzheimer's disease and schizophrenia. Currently, it is not possible to assess NMDAr availability in vivo. The purpose of this study was to develop a positron emission tomography (PET) ligand for the NMDAr ion channel. A series of di- and tri-N-substituted diarylguanidines was synthesized. In addition, in vitro binding affinity for the NMDAr ion channel in rat forebrain membrane fractions was assessed. Compounds 10, 11 and 32 were radiolabeled with either carbon-11 or fluorine-18. Ligands [

Original language	English
Pages (from-to)	1189-1206
Journal	Bioorganic and Medicinal Chemistry
Volume	23
Issue number	5
DOIs	https://doi.org/10.1016/j.bmc.2014.12.029
Publication status	Published - 2015

Access to Document

10.1016/j.bmc.2014.12.029

Persistent URL (handle)

Copy link address

Fingerprint

Dive into the research topics of 'Synthesis, structure activity relationship, radiolabeling and preclinical evaluation of high affinity ligands for the ion channel of the N-methyl-D-aspartate receptor as potential imaging probes for positron emission tomography'. Together they form a unique fingerprint.

Cite this

Klein, P. J., Christiaans, J. A. M., Metaxas, A., Schuit, R. C., Lammertsma, A. A., van Berckel, B. N. M., & Windhorst, A. D. (2015). Synthesis, structure activity relationship, radiolabeling and preclinical evaluation of high affinity ligands for the ion channel of the N-methyl-D-aspartate receptor as potential imaging probes for positron emission tomography. Bioorganic and Medicinal Chemistry, 23(5), 1189-1206. https://doi.org/10.1016/j.bmc.2014.12.029

@article{aa232d65e3c8430bbfbd64893bfa7a10,

title = "Synthesis, structure activity relationship, radiolabeling and preclinical evaluation of high affinity ligands for the ion channel of the N-methyl-D-aspartate receptor as potential imaging probes for positron emission tomography",

abstract = "The N-methyl-d-aspartate receptor (NMDAr) is involved in many neurological and psychiatric disorders including Alzheimer's disease and schizophrenia. Currently, it is not possible to assess NMDAr availability in vivo. The purpose of this study was to develop a positron emission tomography (PET) ligand for the NMDAr ion channel. A series of di- and tri-N-substituted diarylguanidines was synthesized. In addition, in vitro binding affinity for the NMDAr ion channel in rat forebrain membrane fractions was assessed. Compounds 10, 11 and 32 were radiolabeled with either carbon-11 or fluorine-18. Ligands [",

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

year = "2015",

doi = "10.1016/j.bmc.2014.12.029",

language = "English",

volume = "23",

pages = "1189--1206",

journal = "Bioorganic and Medicinal Chemistry",

issn = "0968-0896",

publisher = "Elsevier Limited",

number = "5",

}

Klein, PJ, Christiaans, JAM, Metaxas, A, Schuit, RC, Lammertsma, AA, van Berckel, BNM & Windhorst, AD 2015, 'Synthesis, structure activity relationship, radiolabeling and preclinical evaluation of high affinity ligands for the ion channel of the N-methyl-D-aspartate receptor as potential imaging probes for positron emission tomography', Bioorganic and Medicinal Chemistry, vol. 23, no. 5, pp. 1189-1206. https://doi.org/10.1016/j.bmc.2014.12.029

Synthesis, structure activity relationship, radiolabeling and preclinical evaluation of high affinity ligands for the ion channel of the N-methyl-D-aspartate receptor as potential imaging probes for positron emission tomography. / Klein, P.J.; Christiaans, J.A.M.; Metaxas, A. et al.
In: Bioorganic and Medicinal Chemistry, Vol. 23, No. 5, 2015, p. 1189-1206.

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

TY - JOUR

T1 - Synthesis, structure activity relationship, radiolabeling and preclinical evaluation of high affinity ligands for the ion channel of the N-methyl-D-aspartate receptor as potential imaging probes for positron emission tomography

AU - Klein, P.J.

AU - Christiaans, J.A.M.

AU - Metaxas, A.

AU - Schuit, R.C.

AU - Lammertsma, A.A.

AU - van Berckel, B.N.M.

AU - Windhorst, A.D.

PY - 2015

Y1 - 2015

N2 - The N-methyl-d-aspartate receptor (NMDAr) is involved in many neurological and psychiatric disorders including Alzheimer's disease and schizophrenia. Currently, it is not possible to assess NMDAr availability in vivo. The purpose of this study was to develop a positron emission tomography (PET) ligand for the NMDAr ion channel. A series of di- and tri-N-substituted diarylguanidines was synthesized. In addition, in vitro binding affinity for the NMDAr ion channel in rat forebrain membrane fractions was assessed. Compounds 10, 11 and 32 were radiolabeled with either carbon-11 or fluorine-18. Ligands [

AB - The N-methyl-d-aspartate receptor (NMDAr) is involved in many neurological and psychiatric disorders including Alzheimer's disease and schizophrenia. Currently, it is not possible to assess NMDAr availability in vivo. The purpose of this study was to develop a positron emission tomography (PET) ligand for the NMDAr ion channel. A series of di- and tri-N-substituted diarylguanidines was synthesized. In addition, in vitro binding affinity for the NMDAr ion channel in rat forebrain membrane fractions was assessed. Compounds 10, 11 and 32 were radiolabeled with either carbon-11 or fluorine-18. Ligands [

U2 - 10.1016/j.bmc.2014.12.029

DO - 10.1016/j.bmc.2014.12.029

M3 - Article

SN - 0968-0896

VL - 23

SP - 1189

EP - 1206

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 5

ER -

Klein PJ, Christiaans JAM, Metaxas A, Schuit RC, Lammertsma AA, van Berckel BNM et al. Synthesis, structure activity relationship, radiolabeling and preclinical evaluation of high affinity ligands for the ion channel of the N-methyl-D-aspartate receptor as potential imaging probes for positron emission tomography. Bioorganic and Medicinal Chemistry. 2015;23(5):1189-1206. doi: 10.1016/j.bmc.2014.12.029