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In vivo characteristics of IBZM in rat brains: an agent for quantitative SPECT imaging of dopamine D[sub 2] receptors; Preparation of [sup 125]I-IBZM and its biodistribution and kinetic properties

Abstract

[sup 123]I-(S)-(-)-3-iodo-2-hydroxy-6-methoxy-N-[(1-ethyl-2-pyrrolidinyl) methyl]-benzamide (IBZM) is a CNS dopamine D[sub 2] receptor imaging agent for SPECT and has already been used clinically in the United States, Canada and Europe. However, methods of quantitative SPECT measurement of the D[sub 2] receptor density have not been well established. We performed in vivo biodistribution studies of [sup 125]I-IBZM in rat brains as the first step toward establishment of a basis for quantitative SPECT imaging of D[sub 2] receptors in humans. [sup 125]I-IBZM was prepared by the chloramine-T method. Radiochemical yields were 80 to 90% and radiochemical purity was 94.7% on day 81 after labeling. At 10, 30, 60 and 120 min after injection of the radiopharmaceutical, the percent uptakes (% dose/g) in the rat striatum were 2.9, 1.9, 1.7 and 1.0, respectively. These kinetic data were considered suitable for SPECT imagings. Pretreatment with haloperidol (1 mg/kg) blocked specific striatal uptake and there was a significant reduction in the uptake to 40.9% of the unblocked uptake at 60 min after injection (p=0.006). The regional IBZM uptake ratio of striatum-to-cerebellum increased steadily from 1.7 at 10 min to 5.7 at 120 min. This suggests that SPECT imaging must be done during fixed time after tracer injection  More>>
Publication Date:
May 01, 1994
Product Type:
Journal Article
Reference Number:
JPN-94-007358; EDB-94-126285
Resource Relation:
Journal Name: Kaku Igaku (Japanese Journal of Nuclear Medicine); (Japan); Journal Volume: 31:5
Subject:
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.; BRAIN; RADIONUCLIDE KINETICS; IODINE 125; DOPAMINE; LABELLING; PYRROLIDINES; RATS; RECEPTORS; SINGLE PHOTON EMISSION COMPUTED TOMOGRAPHY; TIME DEPENDENCE; TISSUE DISTRIBUTION; TRANQUILIZERS; UPTAKE; AMINES; ANIMALS; AROMATICS; AUTONOMIC NERVOUS SYSTEM AGENTS; AZOLES; BETA DECAY RADIOISOTOPES; BODY; CARDIOTONICS; CARDIOVASCULAR AGENTS; CENTRAL NERVOUS SYSTEM; CENTRAL NERVOUS SYSTEM AGENTS; COMPUTERIZED TOMOGRAPHY; DAYS LIVING RADIOISOTOPES; DIAGNOSTIC TECHNIQUES; DISTRIBUTION; DRUGS; ELECTRON CAPTURE RADIOISOTOPES; EMISSION COMPUTED TOMOGRAPHY; HETEROCYCLIC COMPOUNDS; HYDROXY COMPOUNDS; INTERMEDIATE MASS NUCLEI; INTERNAL CONVERSION RADIOISOTOPES; IODINE ISOTOPES; ISOTOPES; MAMMALS; MEMBRANE PROTEINS; NERVOUS SYSTEM; NEUROREGULATORS; NUCLEI; ODD-EVEN NUCLEI; ORGANIC COMPOUNDS; ORGANIC NITROGEN COMPOUNDS; ORGANS; PHENOLS; POLYPHENOLS; PROTEINS; PSYCHOTROPIC DRUGS; PYRROLES; RADIOISOTOPES; RODENTS; SYMPATHOMIMETICS; TOMOGRAPHY; VERTEBRATES; 560162* - Radionuclide Effects, Kinetics, & Toxicology- Animals, Plants, Microorganisms, & Cells
OSTI ID:
7143600
Country of Origin:
Japan
Language:
Japanese
Other Identifying Numbers:
Journal ID: ISSN 0022-7854; CODEN: KAIGBZ
Submitting Site:
JPN
Size:
Pages: 513-519
Announcement Date:
Sep 15, 1994

Citation Formats

Matsumura, Kaname, Nakashima, Hiromichi, Nakagawa, Tsuyoshi, Toyama, Hiroshi, Ichise, Masanori, Kurami, Miki, Maeda, Hisato, Takeuchi, Akira, and Koga, Sukehiko. In vivo characteristics of IBZM in rat brains: an agent for quantitative SPECT imaging of dopamine D[sub 2] receptors; Preparation of [sup 125]I-IBZM and its biodistribution and kinetic properties. Japan: N. p., 1994. Web.
Matsumura, Kaname, Nakashima, Hiromichi, Nakagawa, Tsuyoshi, Toyama, Hiroshi, Ichise, Masanori, Kurami, Miki, Maeda, Hisato, Takeuchi, Akira, & Koga, Sukehiko. In vivo characteristics of IBZM in rat brains: an agent for quantitative SPECT imaging of dopamine D[sub 2] receptors; Preparation of [sup 125]I-IBZM and its biodistribution and kinetic properties. Japan.
Matsumura, Kaname, Nakashima, Hiromichi, Nakagawa, Tsuyoshi, Toyama, Hiroshi, Ichise, Masanori, Kurami, Miki, Maeda, Hisato, Takeuchi, Akira, and Koga, Sukehiko. 1994. "In vivo characteristics of IBZM in rat brains: an agent for quantitative SPECT imaging of dopamine D[sub 2] receptors; Preparation of [sup 125]I-IBZM and its biodistribution and kinetic properties." Japan.
@misc{etde_7143600,
title = {In vivo characteristics of IBZM in rat brains: an agent for quantitative SPECT imaging of dopamine D[sub 2] receptors; Preparation of [sup 125]I-IBZM and its biodistribution and kinetic properties}
author = {Matsumura, Kaname, Nakashima, Hiromichi, Nakagawa, Tsuyoshi, Toyama, Hiroshi, Ichise, Masanori, Kurami, Miki, Maeda, Hisato, Takeuchi, Akira, and Koga, Sukehiko}
abstractNote = {[sup 123]I-(S)-(-)-3-iodo-2-hydroxy-6-methoxy-N-[(1-ethyl-2-pyrrolidinyl) methyl]-benzamide (IBZM) is a CNS dopamine D[sub 2] receptor imaging agent for SPECT and has already been used clinically in the United States, Canada and Europe. However, methods of quantitative SPECT measurement of the D[sub 2] receptor density have not been well established. We performed in vivo biodistribution studies of [sup 125]I-IBZM in rat brains as the first step toward establishment of a basis for quantitative SPECT imaging of D[sub 2] receptors in humans. [sup 125]I-IBZM was prepared by the chloramine-T method. Radiochemical yields were 80 to 90% and radiochemical purity was 94.7% on day 81 after labeling. At 10, 30, 60 and 120 min after injection of the radiopharmaceutical, the percent uptakes (% dose/g) in the rat striatum were 2.9, 1.9, 1.7 and 1.0, respectively. These kinetic data were considered suitable for SPECT imagings. Pretreatment with haloperidol (1 mg/kg) blocked specific striatal uptake and there was a significant reduction in the uptake to 40.9% of the unblocked uptake at 60 min after injection (p=0.006). The regional IBZM uptake ratio of striatum-to-cerebellum increased steadily from 1.7 at 10 min to 5.7 at 120 min. This suggests that SPECT imaging must be done during fixed time after tracer injection for the semiquantitative ratio to be meaningful. (author).}
journal = []
volume = {31:5}
journal type = {AC}
place = {Japan}
year = {1994}
month = {May}
}