title: Preclinical studies on [11C]MPDX for mapping adenosine A1 receptors by positron emission tomography.
abstract: In previous in vivo studies with mice, rats and cats, we have demonstrated that [11C]MPDX ([1-methyl-11C]8-dicyclopropylmethyl-1-methyl-3-propylxanthine) is a potential radioligand for mapping adenosine A1 receptors of the brain by positron emission tomography (PET). In the present study, we performed a preclinical study. The radiation absorbed-dose by [11C]MPDX in humans estimated from the tissue distribution in mice was low enough for clinical use, and the acute toxicity and mutagenicity of MPDX were not found. The monkey brain was clearly visualized by PET with [11C]MPDX. We have concluded that [11C]MPDX is suitable for mapping adenosine A1 receptors in the human brain by PET.
authors.affiliation: Positron Medical Center, Tokyo Metropolitan Institute of Gerontology, Japan. ishiwata@pet.tmig.or.jp
authors.forename: Kiichi
authors.initials: K
authors.lastname: Ishiwata
authors.forename: Tadashi
authors.initials: T
authors.lastname: Nariai
authors.forename: Yuichi
authors.initials: Y
authors.lastname: Kimura
authors.forename: Keiichi
authors.initials: K
authors.lastname: Oda
authors.forename: Kazunori
authors.initials: K
authors.lastname: Kawamura
authors.forename: Kenji
authors.initials: K
authors.lastname: Ishii
authors.forename: Michio
authors.initials: M
authors.lastname: Senda
authors.forename: Shinichi
authors.initials: S
authors.lastname: Wakabayashi
authors.forename: Junichi
authors.initials: J
authors.lastname: Shimada
mesh_terms: D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging* / Q000378:metabolism*; D004305:Dose-Response Relationship, Drug; D004307:Dose-Response Relationship, Radiation; D004353:Drug Evaluation, Preclinical; D005260:Female; D006801:Humans; D008253:Macaca mulatta; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D009152:Mutagenicity Tests; D009928:Organ Specificity; D011829:Radiation Dosage; D011874:Radiometry; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics; D051381:Rats; D018047:Receptors, Purinergic P1 / Q000378:metabolism*; D012680:Sensitivity and Specificity; D013045:Species Specificity; D014018:Tissue Distribution; D014055:Tomography, Emission-Computed; D023382:Toxicity Tests, Acute; D019820:Xanthine / Q000493:pharmacokinetics* / Q000633:toxicity*; D014970:Xanthines
chemical_list: C451639:1-methyl-8-dicyclopropylmethyl-1-methyl-3-propylxanthine; D019275:Radiopharmaceuticals; D018047:Receptors, Purinergic P1; D014970:Xanthines; D019820:Xanthine