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[{sup 99m}Tc]TRODAT-1: a novel technetium-99m complex as a dopamine transporter imaging agent

Abstract

Technetium-99m is the most commonly used radionuclide in routine nuclear medicine imaging procedures. Development of {sup 99m}Tc-labeled receptor-specific imaging agents for studying the central nervous system is potentially useful for evaluation of brain function in normal and disease states. A novel {sup 99m}Tc-labeled tropane derivative, [{sup 99m}Tc]TRODAT-1, which is useful as a potential CNS dopamine transporter imaging agent, was evaluated and characterized. After i.v. injection into rats, [{sup 99m}Tc]TRODAT-1 displayed specific brain uptake in the rat striatal region (striatum-cerebellum/cerebellum ratio 1.8 at 60 min), where dopamine neurons are concentrated. The specific striatal uptake could be blocked by pretreating rats with a dose of competing dopamine transporter ligand, {beta}-CIT (or RTI-55, i.v., 1 mg/kg). However, the specific striatal uptake of [{sup 99m}Tc]TRODAT-1 was not affected by co-injection of excess free ligand (TRODAT-1, up to 200 {mu}g per rat) or by pretreating the rats with haloperidol (i.v., 1 mg/kg). The specific uptake in striatal regions of rats that had prior 6-hydroxydopamine lesion in the substantia nigra area showed a dramatic reduction. The radioactive material recovered from the rat striatal homogenates at 60 min after i.v. injection of [{sup 99m}Tc]TRODAT-1 showed primarily the original compound (>95%), a good indication of in vivo stability  More>>
Authors:
Meiping, Kung; [1]  Stevenson, D A; [1]  Ploessl, K; [1]  Meegalla, S K; [1]  Beckwith, A; [1]  Essman, W D; [2]  Mu, M; [1]  Lucki, I; [2]  Kung, H F [1] 
  1. Department of Radiology, University of Pennsylvania, Philadelphia (United States)
  2. Department of Psychiatry, University of Pennsylvania, Philadelphia (United States)
Publication Date:
Apr 01, 1997
Product Type:
Journal Article
Reference Number:
SCA: 550601; PA: DEN-97:0F7970; EDB-97:087749; SN: 97001801508
Resource Relation:
Journal Name: European Journal of Nuclear Medicine; Journal Volume: 24; Journal Issue: 4; Other Information: PBD: Apr 1997
Subject:
55 BIOLOGY AND MEDICINE, BASIC STUDIES; MAMMARY GLANDS; DIAGNOSIS; TECHNETIUM 99; ISOMERIC NUCLEI; LABELLED COMPOUNDS; SENSITIVITY; CARCINOMAS
OSTI ID:
485639
Country of Origin:
Germany
Language:
English
Other Identifying Numbers:
Journal ID: EJNMD9; ISSN 0340-6997; TRN: DE97F7970
Submitting Site:
DEN
Size:
pp. 372-380
Announcement Date:

Citation Formats

Meiping, Kung, Stevenson, D A, Ploessl, K, Meegalla, S K, Beckwith, A, Essman, W D, Mu, M, Lucki, I, and Kung, H F. [{sup 99m}Tc]TRODAT-1: a novel technetium-99m complex as a dopamine transporter imaging agent. Germany: N. p., 1997. Web. doi:10.1007/s002590050065.
Meiping, Kung, Stevenson, D A, Ploessl, K, Meegalla, S K, Beckwith, A, Essman, W D, Mu, M, Lucki, I, & Kung, H F. [{sup 99m}Tc]TRODAT-1: a novel technetium-99m complex as a dopamine transporter imaging agent. Germany. doi:10.1007/s002590050065.
Meiping, Kung, Stevenson, D A, Ploessl, K, Meegalla, S K, Beckwith, A, Essman, W D, Mu, M, Lucki, I, and Kung, H F. 1997. "[{sup 99m}Tc]TRODAT-1: a novel technetium-99m complex as a dopamine transporter imaging agent." Germany. doi:10.1007/s002590050065. https://www.osti.gov/servlets/purl/10.1007/s002590050065.
@misc{etde_485639,
title = {[{sup 99m}Tc]TRODAT-1: a novel technetium-99m complex as a dopamine transporter imaging agent}
author = {Meiping, Kung, Stevenson, D A, Ploessl, K, Meegalla, S K, Beckwith, A, Essman, W D, Mu, M, Lucki, I, and Kung, H F}
abstractNote = {Technetium-99m is the most commonly used radionuclide in routine nuclear medicine imaging procedures. Development of {sup 99m}Tc-labeled receptor-specific imaging agents for studying the central nervous system is potentially useful for evaluation of brain function in normal and disease states. A novel {sup 99m}Tc-labeled tropane derivative, [{sup 99m}Tc]TRODAT-1, which is useful as a potential CNS dopamine transporter imaging agent, was evaluated and characterized. After i.v. injection into rats, [{sup 99m}Tc]TRODAT-1 displayed specific brain uptake in the rat striatal region (striatum-cerebellum/cerebellum ratio 1.8 at 60 min), where dopamine neurons are concentrated. The specific striatal uptake could be blocked by pretreating rats with a dose of competing dopamine transporter ligand, {beta}-CIT (or RTI-55, i.v., 1 mg/kg). However, the specific striatal uptake of [{sup 99m}Tc]TRODAT-1 was not affected by co-injection of excess free ligand (TRODAT-1, up to 200 {mu}g per rat) or by pretreating the rats with haloperidol (i.v., 1 mg/kg). The specific uptake in striatal regions of rats that had prior 6-hydroxydopamine lesion in the substantia nigra area showed a dramatic reduction. The radioactive material recovered from the rat striatal homogenates at 60 min after i.v. injection of [{sup 99m}Tc]TRODAT-1 showed primarily the original compound (>95%), a good indication of in vivo stability in brain tissue. Similar and comparable organ distribution patterns and brain regional uptakes of [{sup 99m}Tc]TRODAT-1 were obtained for male and female rats. (orig./AJ). With 4 figs., 6 tabs.}
doi = {10.1007/s002590050065}
journal = {European Journal of Nuclear Medicine}
issue = {4}
volume = {24}
journal type = {AC}
place = {Germany}
year = {1997}
month = {Apr}
}