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Preclinical studies on [11C]TMSX for mapping adenosine A2A receptors by positron emission tomography

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Abstract

In previousin vivo studies with mice, rats and monkeys, we have demonstrated that [11C]TMSX ([7-methyl-11C]-(E)-8-(3,4,5-trimethoxystyryl)-1,3,7-trimethylxanthine) is a potential radioligang for mapping adenosine A2A receptors of the brain by positron emission tomography (PET). In the present study, we performed a preclinical study. A suitable preparation method for [11C]TMSX injection was established. The radiation absorbed-dose by [11C]TMSX in humans estimated from the tissue distribution in mice was low enough for clinical use, and the acute toxicity and mutagenicity of TMSX were not found. The striatal uptake of [11C]TMSX in mice was reduced by pretreatment with theophylline at the dose of 10 and 100mg/kg, suggesting that the [11C]TMSX PET should be carefully performed in the patients received with theophylline. We have concluded that [11C]TMSX is suitable for mapping adenosine A2A receptors in the human brain by PET.

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Authors and Affiliations

  1. Positron Medical Center, Tokyo Metropolitan Institute of Gerontology, 1-1 Nakacho, Itabashi-ku, 173-0022, Tokyo, Japan

    Kiichi Ishiwata, Wei-Fang Wang, Yuichi Kimura, Kazunori Kawamura & Kenji Ishii

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  1. Kiichi Ishiwata
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  2. Wei-Fang Wang
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  3. Yuichi Kimura
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  4. Kazunori Kawamura
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  5. Kenji Ishii
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Correspondence to Kiichi Ishiwata.

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Ishiwata, K., Wang, WF., Kimura, Y. et al. Preclinical studies on [11C]TMSX for mapping adenosine A2A receptors by positron emission tomography. Ann Nucl Med 17, 205–211 (2003). https://doi.org/10.1007/BF02990023

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  • DOI: https://doi.org/10.1007/BF02990023

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