Two F-18 radiochemistry methods to synthesize a promising transient receptor potential canonical 5 (TRPC5) radioligand

Yanbo Yu; Sandip B. Jadhav; Zhimin Xing; Hao Jiang; Lin Qiu; Tianyu Huang; Joel Perlmutter; Zibo Li; Zhude Tu

doi:10.1016/j.jfluchem.2024.110367

Two F-18 radiochemistry methods to synthesize a promising transient receptor potential canonical 5 (TRPC5) radioligand

Yanbo Yu, Sandip B. Jadhav, Zhimin Xing, Hao Jiang, Lin Qiu, Tianyu Huang, Joel Perlmutter, Zibo Li, Zhude Tu

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

Abstract

TRPC5 is a member of the mammalian transient receptor potential (TRP) channel superfamily and it has been implicated in various physiological and pathological mechanisms of neurological and psychiatric diseases. Fluorine-18 is one of the most widely used radionuclides for PET imaging due to its favorable chemical characteristics and nuclear-physical properties. Herein, we describe two complementary radiosynthetic approaches and preliminary in vivo evaluation for [¹⁸F]TZ78141 as a novel and promising fluorine-18 labeled radiotracer for imaging TRPC5. The latter strategy employed a ruthenium-mediated radiofluorination method, facilitating the rapid synthesis of the desired radiotracer with substantial advantages in simplicity and efficiency.

Original language	English
Article number	110367
Journal	Journal of Fluorine Chemistry
Volume	280
DOIs	https://doi.org/10.1016/j.jfluchem.2024.110367
State	Published - Nov 2024

Keywords

Fluorine -18
PET tracer
Radiolabeling
TRPC5

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10.1016/j.jfluchem.2024.110367

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title = "Two F-18 radiochemistry methods to synthesize a promising transient receptor potential canonical 5 (TRPC5) radioligand",

abstract = "TRPC5 is a member of the mammalian transient receptor potential (TRP) channel superfamily and it has been implicated in various physiological and pathological mechanisms of neurological and psychiatric diseases. Fluorine-18 is one of the most widely used radionuclides for PET imaging due to its favorable chemical characteristics and nuclear-physical properties. Herein, we describe two complementary radiosynthetic approaches and preliminary in vivo evaluation for [18F]TZ78141 as a novel and promising fluorine-18 labeled radiotracer for imaging TRPC5. The latter strategy employed a ruthenium-mediated radiofluorination method, facilitating the rapid synthesis of the desired radiotracer with substantial advantages in simplicity and efficiency.",

keywords = "Fluorine -18, PET tracer, Radiolabeling, TRPC5",

author = "Yanbo Yu and Jadhav, {Sandip B.} and Zhimin Xing and Hao Jiang and Lin Qiu and Tianyu Huang and Joel Perlmutter and Zibo Li and Zhude Tu",

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year = "2024",

month = nov,

doi = "10.1016/j.jfluchem.2024.110367",

language = "English",

volume = "280",

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TY - JOUR

T1 - Two F-18 radiochemistry methods to synthesize a promising transient receptor potential canonical 5 (TRPC5) radioligand

AU - Yu, Yanbo

AU - Jadhav, Sandip B.

AU - Xing, Zhimin

AU - Jiang, Hao

AU - Qiu, Lin

AU - Huang, Tianyu

AU - Perlmutter, Joel

AU - Li, Zibo

AU - Tu, Zhude

PY - 2024/11

Y1 - 2024/11

N2 - TRPC5 is a member of the mammalian transient receptor potential (TRP) channel superfamily and it has been implicated in various physiological and pathological mechanisms of neurological and psychiatric diseases. Fluorine-18 is one of the most widely used radionuclides for PET imaging due to its favorable chemical characteristics and nuclear-physical properties. Herein, we describe two complementary radiosynthetic approaches and preliminary in vivo evaluation for [18F]TZ78141 as a novel and promising fluorine-18 labeled radiotracer for imaging TRPC5. The latter strategy employed a ruthenium-mediated radiofluorination method, facilitating the rapid synthesis of the desired radiotracer with substantial advantages in simplicity and efficiency.

AB - TRPC5 is a member of the mammalian transient receptor potential (TRP) channel superfamily and it has been implicated in various physiological and pathological mechanisms of neurological and psychiatric diseases. Fluorine-18 is one of the most widely used radionuclides for PET imaging due to its favorable chemical characteristics and nuclear-physical properties. Herein, we describe two complementary radiosynthetic approaches and preliminary in vivo evaluation for [18F]TZ78141 as a novel and promising fluorine-18 labeled radiotracer for imaging TRPC5. The latter strategy employed a ruthenium-mediated radiofluorination method, facilitating the rapid synthesis of the desired radiotracer with substantial advantages in simplicity and efficiency.

KW - Fluorine -18

KW - PET tracer

KW - Radiolabeling

KW - TRPC5

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U2 - 10.1016/j.jfluchem.2024.110367

DO - 10.1016/j.jfluchem.2024.110367

M3 - Article

AN - SCOPUS:85207281504

SN - 0022-1139

VL - 280

JO - Journal of Fluorine Chemistry

JF - Journal of Fluorine Chemistry

M1 - 110367

ER -

Two F-18 radiochemistry methods to synthesize a promising transient receptor potential canonical 5 (TRPC5) radioligand

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Keywords

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