Radiolabeling of [11C]FPS-ZM1, a receptor for advanced glycation end products-targeting positron emission tomography radiotracer, using a [11C]CO2-to-[11C]CO chemical conversion

Federico Luzi; Vilius Savickas; Carlotta Taddei; Stefan Hader; Nisha Singh; Antony D Gee; Salvatore Bongarzone

doi:10.4155/fmc-2019-0329

Radiolabeling of [11C]FPS-ZM1, a receptor for advanced glycation end products-targeting positron emission tomography radiotracer, using a [11C]CO2-to-[11C]CO chemical conversion

Federico Luzi, Vilius Savickas, Carlotta Taddei, Stefan Hader, Nisha Singh, Antony D Gee, Salvatore Bongarzone

National Institute for Health Research Biomedical Research Centre at Guy's & St Thomas' NHS Foundation Trust & King's College London, 16th Floor, Tower Wing, Guy's Hospital, Great Maze Pond, London, SE1 9RT, UK.

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Abstract

Aim: The receptor for advanced glycation end products (RAGE) is a viable target for early Alzheimer's disease (AD) diagnosis using positron emission tomography (PET) as RAGE overexpression precedes Aβ plaque formation. The development of a carbon-11 analog of FPS-ZM1 (N-benzyl-4-chloro-N-cyclohexylbenzamide, [11C]FPS-ZM1), possessing nanomolar affinity for RAGE, may enable the imaging of RAGE for early AD detection.

Methodology & results: Herein we report an optimized [11C]CO2-to-[11C]CO chemical conversion for the synthesis of [11C]FPS-ZM1 and in vitro brain autoradiography. The [11C]CO2-to-[11C]CO conversion via 11C-silanecarboxylate derivatives was achieved with a 57% yield within 30 s from end of [11C]CO2 delivery. [11C]FPS-ZM1 was obtained with a decay-corrected isolated radiochemical yield of 9.5%.

Conclusion: [11C]FPS-ZM1 distribution in brain tissues of wild-type versus transgenic AD model mice showed no statistically significant difference and high nondisplaceable binding.

Original language	English
Pages (from-to)	511-521
Number of pages	11
Journal	Future Medicinal Chemistry
Volume	12
Issue number	6
Early online date	27 Feb 2020
DOIs	https://doi.org/10.4155/fmc-2019-0329
Publication status	Published - Mar 2020

Keywords

Alzheimer’s disease
FPS-ZM1
PET imaging
RAGE
[11C]CO radiochemistry
carbon-11
silanecarboxylate derivatives

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10.4155/fmc-2019-0329

Radiolabeling of [11C]FPS-ZM1_Accepted7Jan2020_ePublished27Feb2020_GREEN AAMAccepted author manuscript, 702 KB

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@article{cf1f6d37a45747d0a64f2974a893ec20,

title = "Radiolabeling of [11C]FPS-ZM1, a receptor for advanced glycation end products-targeting positron emission tomography radiotracer, using a [11C]CO2-to-[11C]CO chemical conversion",

abstract = "Aim: The receptor for advanced glycation end products (RAGE) is a viable target for early Alzheimer's disease (AD) diagnosis using positron emission tomography (PET) as RAGE overexpression precedes Aβ plaque formation. The development of a carbon-11 analog of FPS-ZM1 (N-benzyl-4-chloro-N-cyclohexylbenzamide, [11C]FPS-ZM1), possessing nanomolar affinity for RAGE, may enable the imaging of RAGE for early AD detection.Methodology & results: Herein we report an optimized [11C]CO2-to-[11C]CO chemical conversion for the synthesis of [11C]FPS-ZM1 and in vitro brain autoradiography. The [11C]CO2-to-[11C]CO conversion via 11C-silanecarboxylate derivatives was achieved with a 57% yield within 30 s from end of [11C]CO2 delivery. [11C]FPS-ZM1 was obtained with a decay-corrected isolated radiochemical yield of 9.5%.Conclusion: [11C]FPS-ZM1 distribution in brain tissues of wild-type versus transgenic AD model mice showed no statistically significant difference and high nondisplaceable binding.",

keywords = "Alzheimer{\textquoteright}s disease, FPS-ZM1, PET imaging, RAGE, [11C]CO radiochemistry, carbon-11, silanecarboxylate derivatives",

author = "Federico Luzi and Vilius Savickas and Carlotta Taddei and Stefan Hader and Nisha Singh and Gee, {Antony D} and Salvatore Bongarzone",

year = "2020",

month = mar,

doi = "10.4155/fmc-2019-0329",

language = "English",

volume = "12",

pages = "511--521",

journal = "Future Medicinal Chemistry",

issn = "1756-8927",

publisher = "Newlands Press",

number = "6",

}

Radiolabeling of [11C]FPS-ZM1, a receptor for advanced glycation end products-targeting positron emission tomography radiotracer, using a [11C]CO2-to-[11C]CO chemical conversion. / Luzi, Federico; Savickas, Vilius; Taddei, Carlotta et al.
In: Future Medicinal Chemistry, Vol. 12, No. 6, 03.2020, p. 511-521.

Research output: Contribution to journal › Article › peer-review

TY - JOUR

T1 - Radiolabeling of [11C]FPS-ZM1, a receptor for advanced glycation end products-targeting positron emission tomography radiotracer, using a [11C]CO2-to-[11C]CO chemical conversion

AU - Luzi, Federico

AU - Savickas, Vilius

AU - Taddei, Carlotta

AU - Hader, Stefan

AU - Singh, Nisha

AU - Gee, Antony D

AU - Bongarzone, Salvatore

PY - 2020/3

Y1 - 2020/3

N2 - Aim: The receptor for advanced glycation end products (RAGE) is a viable target for early Alzheimer's disease (AD) diagnosis using positron emission tomography (PET) as RAGE overexpression precedes Aβ plaque formation. The development of a carbon-11 analog of FPS-ZM1 (N-benzyl-4-chloro-N-cyclohexylbenzamide, [11C]FPS-ZM1), possessing nanomolar affinity for RAGE, may enable the imaging of RAGE for early AD detection.Methodology & results: Herein we report an optimized [11C]CO2-to-[11C]CO chemical conversion for the synthesis of [11C]FPS-ZM1 and in vitro brain autoradiography. The [11C]CO2-to-[11C]CO conversion via 11C-silanecarboxylate derivatives was achieved with a 57% yield within 30 s from end of [11C]CO2 delivery. [11C]FPS-ZM1 was obtained with a decay-corrected isolated radiochemical yield of 9.5%.Conclusion: [11C]FPS-ZM1 distribution in brain tissues of wild-type versus transgenic AD model mice showed no statistically significant difference and high nondisplaceable binding.

AB - Aim: The receptor for advanced glycation end products (RAGE) is a viable target for early Alzheimer's disease (AD) diagnosis using positron emission tomography (PET) as RAGE overexpression precedes Aβ plaque formation. The development of a carbon-11 analog of FPS-ZM1 (N-benzyl-4-chloro-N-cyclohexylbenzamide, [11C]FPS-ZM1), possessing nanomolar affinity for RAGE, may enable the imaging of RAGE for early AD detection.Methodology & results: Herein we report an optimized [11C]CO2-to-[11C]CO chemical conversion for the synthesis of [11C]FPS-ZM1 and in vitro brain autoradiography. The [11C]CO2-to-[11C]CO conversion via 11C-silanecarboxylate derivatives was achieved with a 57% yield within 30 s from end of [11C]CO2 delivery. [11C]FPS-ZM1 was obtained with a decay-corrected isolated radiochemical yield of 9.5%.Conclusion: [11C]FPS-ZM1 distribution in brain tissues of wild-type versus transgenic AD model mice showed no statistically significant difference and high nondisplaceable binding.

KW - Alzheimer’s disease

KW - FPS-ZM1

KW - PET imaging

KW - RAGE

KW - [11C]CO radiochemistry

KW - carbon-11

KW - silanecarboxylate derivatives

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U2 - 10.4155/fmc-2019-0329

DO - 10.4155/fmc-2019-0329

M3 - Article

C2 - 32100545

SN - 1756-8927

VL - 12

SP - 511

EP - 521

JO - Future Medicinal Chemistry

JF - Future Medicinal Chemistry

IS - 6

ER -

Radiolabeling of [11C]FPS-ZM1, a receptor for advanced glycation end products-targeting positron emission tomography radiotracer, using a [11C]CO2-to-[11C]CO chemical conversion

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