Radiosynthesis and biological evaluation of a promising σ2-receptor ligand radiolabeled with fluorine-18 or iodine-125 as a PET/SPECT probe for imaging breast cancer

Zhude Tu; Jinbin Xu; Lynne A. Jones; Shihong Li; Dexing Zeng; Mei Ping Kung; Hank F. Kung; Robert H. Mach

doi:10.1016/j.apradiso.2010.06.004

Radiosynthesis and biological evaluation of a promising σ₂-receptor ligand radiolabeled with fluorine-18 or iodine-125 as a PET/SPECT probe for imaging breast cancer

Zhude Tu, Jinbin Xu, Lynne A. Jones, Shihong Li, Dexing Zeng, Mei Ping Kung, Hank F. Kung, Robert H. Mach

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

31 Scopus citations

Abstract

Sigma-2 receptors represent an endogenous marker for proliferation in solid tumors. The high affinity, high selectivity σ₂ receptor ligand N-(4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)butyl)-2-(2-fluoroethoxy)-5-iodo-3-methoxybenzamide (3) was separately radiolabeled with F-18 and I-125. The radiolabeling yield was 30% and 70% for [¹⁸F]3 and [¹²⁵I]3, respectively. Studies of [¹²⁵I]3 using murine 66 breast tumor membrane homogenates and evaluation of [¹⁸F]3 and [¹²⁵I]3 in 66 tumor-bearing mice indicate that this ligand has potential as a PET or a SPECT probe for imaging σ₂ receptors in breast cancer.

Original language	English
Pages (from-to)	2268-2273
Number of pages	6
Journal	Applied Radiation and Isotopes
Volume	68
Issue number	12
DOIs	https://doi.org/10.1016/j.apradiso.2010.06.004
State	Published - Dec 2010

Keywords

Breast cancer
F-18
I-125
Molecular imaging
Sigma receptor

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10.1016/j.apradiso.2010.06.004

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title = "Radiosynthesis and biological evaluation of a promising σ2-receptor ligand radiolabeled with fluorine-18 or iodine-125 as a PET/SPECT probe for imaging breast cancer",

abstract = "Sigma-2 receptors represent an endogenous marker for proliferation in solid tumors. The high affinity, high selectivity σ2 receptor ligand N-(4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)butyl)-2-(2-fluoroethoxy)-5-iodo-3-methoxybenzamide (3) was separately radiolabeled with F-18 and I-125. The radiolabeling yield was 30% and 70% for [18F]3 and [125I]3, respectively. Studies of [125I]3 using murine 66 breast tumor membrane homogenates and evaluation of [18F]3 and [125I]3 in 66 tumor-bearing mice indicate that this ligand has potential as a PET or a SPECT probe for imaging σ2 receptors in breast cancer.",

keywords = "Breast cancer, F-18, I-125, Molecular imaging, Sigma receptor",

author = "Zhude Tu and Jinbin Xu and Jones, {Lynne A.} and Shihong Li and Dexing Zeng and Kung, {Mei Ping} and Kung, {Hank F.} and Mach, {Robert H.}",

note = "Funding Information: This research was supported by the following grants: National Cancer Institute (NCI) Grant CA-102869 (Mach, PI) and DAMD17-01-1-0446 (Mach, PI) awarded by the Department of Defense (DOD) Breast Cancer Research Program (BCRP) of the US Army Medical Research and Material Command Office.",

year = "2010",

month = dec,

doi = "10.1016/j.apradiso.2010.06.004",

language = "English",

volume = "68",

pages = "2268--2273",

journal = "Applied Radiation and Isotopes",

issn = "0969-8043",

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T1 - Radiosynthesis and biological evaluation of a promising σ2-receptor ligand radiolabeled with fluorine-18 or iodine-125 as a PET/SPECT probe for imaging breast cancer

AU - Tu, Zhude

AU - Xu, Jinbin

AU - Jones, Lynne A.

AU - Li, Shihong

AU - Zeng, Dexing

AU - Kung, Mei Ping

AU - Kung, Hank F.

AU - Mach, Robert H.

N1 - Funding Information: This research was supported by the following grants: National Cancer Institute (NCI) Grant CA-102869 (Mach, PI) and DAMD17-01-1-0446 (Mach, PI) awarded by the Department of Defense (DOD) Breast Cancer Research Program (BCRP) of the US Army Medical Research and Material Command Office.

PY - 2010/12

Y1 - 2010/12

N2 - Sigma-2 receptors represent an endogenous marker for proliferation in solid tumors. The high affinity, high selectivity σ2 receptor ligand N-(4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)butyl)-2-(2-fluoroethoxy)-5-iodo-3-methoxybenzamide (3) was separately radiolabeled with F-18 and I-125. The radiolabeling yield was 30% and 70% for [18F]3 and [125I]3, respectively. Studies of [125I]3 using murine 66 breast tumor membrane homogenates and evaluation of [18F]3 and [125I]3 in 66 tumor-bearing mice indicate that this ligand has potential as a PET or a SPECT probe for imaging σ2 receptors in breast cancer.

AB - Sigma-2 receptors represent an endogenous marker for proliferation in solid tumors. The high affinity, high selectivity σ2 receptor ligand N-(4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)butyl)-2-(2-fluoroethoxy)-5-iodo-3-methoxybenzamide (3) was separately radiolabeled with F-18 and I-125. The radiolabeling yield was 30% and 70% for [18F]3 and [125I]3, respectively. Studies of [125I]3 using murine 66 breast tumor membrane homogenates and evaluation of [18F]3 and [125I]3 in 66 tumor-bearing mice indicate that this ligand has potential as a PET or a SPECT probe for imaging σ2 receptors in breast cancer.

KW - Breast cancer

KW - F-18

KW - I-125

KW - Molecular imaging

KW - Sigma receptor

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DO - 10.1016/j.apradiso.2010.06.004

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AN - SCOPUS:77956408380

SN - 0969-8043

VL - 68

SP - 2268

EP - 2273

JO - Applied Radiation and Isotopes

JF - Applied Radiation and Isotopes

IS - 12

ER -

Radiosynthesis and biological evaluation of a promising σ₂-receptor ligand radiolabeled with fluorine-18 or iodine-125 as a PET/SPECT probe for imaging breast cancer

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