Rapid, high-yield enzymatic synthesis of n.c.a. 6-[18F]fluorodopamine (6-[18F]FDA) for in vivo application

Karsten Bamminger; Julia Raitanen; Georgios Karanikas; Sazan Rasul; Lukas Nics; Markus Mitterhauser; Wolfgang Wadsak; Marcus Hacker; Verena Pichler; Chrysoula Vraka

doi:10.1016/j.nucmedbio.2022.07.001

Rapid, high-yield enzymatic synthesis of n.c.a. 6-[¹⁸F]fluorodopamine (6-[¹⁸F]FDA) for in vivo application

Karsten Bamminger
, Julia Raitanen
, Georgios Karanikas
, Sazan Rasul
, Lukas Nics
, Markus Mitterhauser
, Wolfgang Wadsak
, Marcus Hacker
, Verena Pichler
, Chrysoula Vraka

Department of Pharmaceutical Sciences

Publications: Contribution to journal › Article › Peer Reviewed

Abstract

6-[¹⁸F]Fluorodopamine (6-[¹⁸F]FDA) proved valuable as a diagnostic tool for neuroendocrine and rare tumors, such as ganglioneuromas and pheochromocytomas, however, clinical application is still limited. So far, its radiosyntheses were impeded by the formation of side-products, low molar activity, multi-step reactions and the use of challenging precursors. Here, we describe a detailed enzymatic procedure for fast, simple and high yield synthesis of no carrier added 6-[¹⁸F]FDA from 6-[¹⁸F]FDOPA with high radiochemical yield of ~69 % and >95 % purity as determined by radio-HPLC and -TLC. The product formulation was stable and suitable for in vivo application.

Original language	English
Pages (from-to)	189-197
Number of pages	9
Journal	Nuclear Medicine and Biology
Volume	114-115
DOIs	https://doi.org/10.1016/j.nucmedbio.2022.07.001
Publication status	Published - 1 Nov 2022

Funding

We thank Irene Klag for her pre-work on enzymatic synthesis and we are grateful to Eva-Maria Klebermass, Angelika Schmidt and Susanne Feix for their administrative support. We also like to thank Thomas Zenz for his technical support. This research did not receive any specific grant from funding agencies in the public, commercial, or not-for-profit sectors.

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Austrian Fields of Science 2012

104020 Radiochemistry

Keywords

6-FDOPA
6-fluorodopamine
Enzymatic
Fluorine-18
Radiosynthesis
Tyrosine decarboxylase

Access to Document

10.1016/j.nucmedbio.2022.07.001Licence: CC BY 4.0

https://phaidra.univie.ac.at/o:1646671Licence: CC BY 4.0

Cite this

@article{27c21448cf30477e90af09715dd5903d,

title = "Rapid, high-yield enzymatic synthesis of n.c.a. 6-[18F]fluorodopamine (6-[18F]FDA) for in vivo application",

abstract = "6-[18F]Fluorodopamine (6-[18F]FDA) proved valuable as a diagnostic tool for neuroendocrine and rare tumors, such as ganglioneuromas and pheochromocytomas, however, clinical application is still limited. So far, its radiosyntheses were impeded by the formation of side-products, low molar activity, multi-step reactions and the use of challenging precursors. Here, we describe a detailed enzymatic procedure for fast, simple and high yield synthesis of no carrier added 6-[18F]FDA from 6-[18F]FDOPA with high radiochemical yield of \textasciitilde{}69 \% and >95 \% purity as determined by radio-HPLC and -TLC. The product formulation was stable and suitable for in vivo application.",

keywords = "6-FDOPA, 6-fluorodopamine, Enzymatic, Fluorine-18, Radiosynthesis, Tyrosine decarboxylase",

author = "Karsten Bamminger and Julia Raitanen and Georgios Karanikas and Sazan Rasul and Lukas Nics and Markus Mitterhauser and Wolfgang Wadsak and Marcus Hacker and Verena Pichler and Chrysoula Vraka",

note = "Funding Information: We thank Irene Klag for her pre-work on enzymatic synthesis and we are grateful to Eva-Maria Klebermass, Angelika Schmidt and Susanne Feix for their administrative support. We also like to thank Thomas Zenz for his technical support. This research did not receive any specific grant from funding agencies in the public, commercial, or not-for-profit sectors. Publisher Copyright: {\textcopyright} 2022",

year = "2022",

month = nov,

day = "1",

doi = "10.1016/j.nucmedbio.2022.07.001",

language = "English",

volume = "114-115",

pages = "189--197",

journal = "Nuclear Medicine and Biology",

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TY - JOUR

T1 - Rapid, high-yield enzymatic synthesis of n.c.a. 6-[18F]fluorodopamine (6-[18F]FDA) for in vivo application

AU - Bamminger, Karsten

AU - Raitanen, Julia

AU - Karanikas, Georgios

AU - Rasul, Sazan

AU - Nics, Lukas

AU - Mitterhauser, Markus

AU - Wadsak, Wolfgang

AU - Hacker, Marcus

AU - Pichler, Verena

AU - Vraka, Chrysoula

N1 - Funding Information: We thank Irene Klag for her pre-work on enzymatic synthesis and we are grateful to Eva-Maria Klebermass, Angelika Schmidt and Susanne Feix for their administrative support. We also like to thank Thomas Zenz for his technical support. This research did not receive any specific grant from funding agencies in the public, commercial, or not-for-profit sectors. Publisher Copyright: © 2022

PY - 2022/11/1

Y1 - 2022/11/1

N2 - 6-[18F]Fluorodopamine (6-[18F]FDA) proved valuable as a diagnostic tool for neuroendocrine and rare tumors, such as ganglioneuromas and pheochromocytomas, however, clinical application is still limited. So far, its radiosyntheses were impeded by the formation of side-products, low molar activity, multi-step reactions and the use of challenging precursors. Here, we describe a detailed enzymatic procedure for fast, simple and high yield synthesis of no carrier added 6-[18F]FDA from 6-[18F]FDOPA with high radiochemical yield of ~69 % and >95 % purity as determined by radio-HPLC and -TLC. The product formulation was stable and suitable for in vivo application.

AB - 6-[18F]Fluorodopamine (6-[18F]FDA) proved valuable as a diagnostic tool for neuroendocrine and rare tumors, such as ganglioneuromas and pheochromocytomas, however, clinical application is still limited. So far, its radiosyntheses were impeded by the formation of side-products, low molar activity, multi-step reactions and the use of challenging precursors. Here, we describe a detailed enzymatic procedure for fast, simple and high yield synthesis of no carrier added 6-[18F]FDA from 6-[18F]FDOPA with high radiochemical yield of ~69 % and >95 % purity as determined by radio-HPLC and -TLC. The product formulation was stable and suitable for in vivo application.

KW - 6-FDOPA

KW - 6-fluorodopamine

KW - Enzymatic

KW - Fluorine-18

KW - Radiosynthesis

KW - Tyrosine decarboxylase

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