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Occupancy of dopamine transporter and
 the effect of dopamine reuptake inhibition
 by mazindol in living human brain

https://repo.qst.go.jp/records/71157
https://repo.qst.go.jp/records/71157
09b833af-08d8-40ed-a943-bba5ae632a50
Item type 会議発表用資料 / Presentation(1)
公開日 2013-06-18
タイトル
タイトル Occupancy of dopamine transporter and
 the effect of dopamine reuptake inhibition
 by mazindol in living human brain
言語
言語 eng
資源タイプ
資源タイプ識別子 http://purl.org/coar/resource_type/c_c94f
資源タイプ conference object
アクセス権
アクセス権 metadata only access
アクセス権URI http://purl.org/coar/access_right/c_14cb
著者 Kimura, Yasuyuki

× Kimura, Yasuyuki

WEKO 699540

Kimura, Yasuyuki

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Ito, Hiroshi

× Ito, Hiroshi

WEKO 699541

Ito, Hiroshi

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Maeda, Jun

× Maeda, Jun

WEKO 699542

Maeda, Jun

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Yamada, Makiko

× Yamada, Makiko

WEKO 699543

Yamada, Makiko

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Fujiwara, Hironobu

× Fujiwara, Hironobu

WEKO 699544

Fujiwara, Hironobu

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Eguchi, Yoko

× Eguchi, Yoko

WEKO 699545

Eguchi, Yoko

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Seki, Chie

× Seki, Chie

WEKO 699546

Seki, Chie

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Kodaka, Fumitoshi

× Kodaka, Fumitoshi

WEKO 699547

Kodaka, Fumitoshi

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Takahata, Keisuke

× Takahata, Keisuke

WEKO 699548

Takahata, Keisuke

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Takano, Harumasa

× Takano, Harumasa

WEKO 699549

Takano, Harumasa

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Ikoma, Youko

× Ikoma, Youko

WEKO 699550

Ikoma, Youko

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Minamimoto, Takafumi

× Minamimoto, Takafumi

WEKO 699551

Minamimoto, Takafumi

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Higuchi, Makoto

× Higuchi, Makoto

WEKO 699552

Higuchi, Makoto

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Suhara, Tetsuya

× Suhara, Tetsuya

WEKO 699553

Suhara, Tetsuya

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木村 泰之

× 木村 泰之

WEKO 699554

en 木村 泰之

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伊藤 浩

× 伊藤 浩

WEKO 699555

en 伊藤 浩

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前田 純

× 前田 純

WEKO 699556

en 前田 純

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山田 真希子

× 山田 真希子

WEKO 699557

en 山田 真希子

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藤原 広臨

× 藤原 広臨

WEKO 699558

en 藤原 広臨

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江口 洋子

× 江口 洋子

WEKO 699559

en 江口 洋子

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関 千江

× 関 千江

WEKO 699560

en 関 千江

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小高 文聰

× 小高 文聰

WEKO 699561

en 小高 文聰

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高畑 圭輔

× 高畑 圭輔

WEKO 699562

en 高畑 圭輔

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高野 晴成

× 高野 晴成

WEKO 699563

en 高野 晴成

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生駒 洋子

× 生駒 洋子

WEKO 699564

en 生駒 洋子

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南本 敬史

× 南本 敬史

WEKO 699565

en 南本 敬史

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樋口 真人

× 樋口 真人

WEKO 699566

en 樋口 真人

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須原 哲也

× 須原 哲也

WEKO 699567

en 須原 哲也

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抄録
内容記述タイプ Abstract
内容記述 Regional alterations in extracellular dopamine levels can be observed in the striatum during performance of neuropsychological tasks using PET1. To increase detection of the alteration, dopamine reuptake inhibitor could be useful for producing a greater magnitude of change in 11C-raclopride binding2. Mazindol is a non-selective catecholamine reuptake inhibitor, which blocks dopamine reuptake and thus could be used as an enhancer of dopamine release by neuropsyhological tasks3. To investigate basic potency of mazindol in human, we measured occupancy of the dopamine transporter and change in 11C-raclopride binding using PET after single oral administration of mazindol.
Methods:
Two sets of PET scans were acquired on six healthy volunteers after oral administration of placebo and 1.5 mg of mazindol. 11C-raclopride was injected at 3 hours after the administration of placebo or mazindol, and 18F-FE-PE2I was injected at 5 hours. In the brain, preset volumes of interest were applied on the spatially normalized PET images. Binding potential of sub-regions of striatum was calculated by the simplified reference tissue model using cerebellum as reference region. Dopamine transporter occupancy was calculated by the % change of the binding potential of 18F-FE-PE2I, and change in extracellular dopamine levels was measured by the % change of that of 11C-raclopride.
Results:
After oral administration of 1.5 mg of mazindol, the binding potential of 18F-FE-PE2I significantly reduced by 20 &#8211; 25 % (p < 0.01, paired t-test), indicating 20 &#8211; 25 % of dopamine transporters in the striatum was occupied by mazindol. Meanwhile, the binding potential of 11C-raclopride reduced by 4 &#8211; 6%, but the reduction was not significant, indicating the change in extracellular dopamine levels by mazindol without neuropsyhological tasks was small. The correlation between the occupancy of dopamine transporter and the change in 11C-raclopride binding was not significant, but there seemed a tendency that the occupancy was negatively related to the change in 11C-raclopride binding among subjects in the associative striatum.
Conclusions:
After oral administration of 1.5 mg of mazindol, dopamine transporters were occupied in a small proportion, and the change in extracellular dopamine levels was minimal. Further studies with a larger sample size would be needed to investigate the relationship between the occupancy of dopamine transporter and the change in extracellular dopamine levels by oral administration of mazindol.
会議概要(会議名, 開催地, 会期, 主催者等)
内容記述タイプ Other
内容記述 Society of Nuclear Medicine and Molecular Imaging 2013 Annual Meeting
発表年月日
日付 2013-06-12
日付タイプ Issued
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