In vivo characteristics of IBZM in rat brains

An agent for quantitative SPECT imaging of dopamine D2 receptors. Preparation of 125I-IBZM and its biodistribution and kinetic properties

K. Matsumura, Hiroshi Toyama, H. Nakashima, M. Ichise, M. Kurami, T. Nakagawa, H. Maeda, A. Takeuchi, S. Koga

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

123I-(S)-(-)-3-iodo-2-hydroxy-6-methoxy-N-[(1 ethyl-2-pyrrolidinyl)methyl]-benzamide (IBZM) is a CNS dopamine D2 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 D2 receptor density have not been well established. We performed in vivo biodistribution studies of 125I-IBZM in rat brains as the first step toward establishment of a basis for quantitative SPECT imaging of D2 receptors in humans. 125I-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.

Original languageEnglish
Pages (from-to)513-519
Number of pages7
JournalKakuigaku
Volume31
Issue number5
Publication statusPublished - 01-01-1994
Externally publishedYes

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Dopamine D2 Receptors
Single-Photon Emission-Computed Tomography
Brain
Injections
Corpus Striatum
Radiopharmaceuticals
Haloperidol
Cerebellum
Canada
3-iodo-2-hydroxy-6-methoxy-N-((1-ethyl-2-pyrrolidinyl)methyl)benzamide

All Science Journal Classification (ASJC) codes

  • Radiology Nuclear Medicine and imaging

Cite this

Matsumura, K. ; Toyama, Hiroshi ; Nakashima, H. ; Ichise, M. ; Kurami, M. ; Nakagawa, T. ; Maeda, H. ; Takeuchi, A. ; Koga, S. / In vivo characteristics of IBZM in rat brains : An agent for quantitative SPECT imaging of dopamine D2 receptors. Preparation of 125I-IBZM and its biodistribution and kinetic properties. In: Kakuigaku. 1994 ; Vol. 31, No. 5. pp. 513-519.
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abstract = "123I-(S)-(-)-3-iodo-2-hydroxy-6-methoxy-N-[(1 ethyl-2-pyrrolidinyl)methyl]-benzamide (IBZM) is a CNS dopamine D2 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 D2 receptor density have not been well established. We performed in vivo biodistribution studies of 125I-IBZM in rat brains as the first step toward establishment of a basis for quantitative SPECT imaging of D2 receptors in humans. 125I-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.",
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In vivo characteristics of IBZM in rat brains : An agent for quantitative SPECT imaging of dopamine D2 receptors. Preparation of 125I-IBZM and its biodistribution and kinetic properties. / Matsumura, K.; Toyama, Hiroshi; Nakashima, H.; Ichise, M.; Kurami, M.; Nakagawa, T.; Maeda, H.; Takeuchi, A.; Koga, S.

In: Kakuigaku, Vol. 31, No. 5, 01.01.1994, p. 513-519.

Research output: Contribution to journalArticle

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T1 - In vivo characteristics of IBZM in rat brains

T2 - An agent for quantitative SPECT imaging of dopamine D2 receptors. Preparation of 125I-IBZM and its biodistribution and kinetic properties

AU - Matsumura, K.

AU - Toyama, Hiroshi

AU - Nakashima, H.

AU - Ichise, M.

AU - Kurami, M.

AU - Nakagawa, T.

AU - Maeda, H.

AU - Takeuchi, A.

AU - Koga, S.

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N2 - 123I-(S)-(-)-3-iodo-2-hydroxy-6-methoxy-N-[(1 ethyl-2-pyrrolidinyl)methyl]-benzamide (IBZM) is a CNS dopamine D2 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 D2 receptor density have not been well established. We performed in vivo biodistribution studies of 125I-IBZM in rat brains as the first step toward establishment of a basis for quantitative SPECT imaging of D2 receptors in humans. 125I-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.

AB - 123I-(S)-(-)-3-iodo-2-hydroxy-6-methoxy-N-[(1 ethyl-2-pyrrolidinyl)methyl]-benzamide (IBZM) is a CNS dopamine D2 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 D2 receptor density have not been well established. We performed in vivo biodistribution studies of 125I-IBZM in rat brains as the first step toward establishment of a basis for quantitative SPECT imaging of D2 receptors in humans. 125I-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.

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