Shin-Ichi Ishii

Tokyo Metropolitan Institute of Gerontology, Edo, Tōkyō, Japan

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Publications (32)52.99 Total impact

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    ABSTRACT: We prepared sigma(1)-receptor selective 1-([4-methoxy-(11)C]-3,4-dimethoxyphenethyl)-4-(3-phenylpropyl)piperazine ([(11)C]SA4503) and its fluorinated analog 1-([4-methoxy-(11)C]3,4-dimethoxyphenethyl)-4-[3-(4-fluorophenyl)propyl]piperazine ([(11)C]SA5845), and their [(11)C]ethoxy and [(18)F]fluoroethoxy analogs, and evaluated their potential for positron emission tomography studies. [(11)C]SA4503 is most selective for sigma(1) receptors, and the other five showed affinities for sigma(1) and sigma(2) receptors with a different extent. All radioligands showed the receptor-specific binding in the brain, and visualized similar regional brain distributions by ex vivo autoradiography. The [(11)C]ethoxy analogs were relatively labile for metabolism.
    Nuclear Medicine and Biology 05/2003; 30(3):273-84. DOI:10.1016/S0969-8051(02)00439-0 · 2.41 Impact Factor
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    ABSTRACT: We prepared an (11)C-labeled adenosine transporter blocker, [1-methyl-(11)C]-3-[1-(6,7-dimethoxyquinazolin-4-yl)piperidin-4-yl]-1,6-dimethyl-2,4(1H, 3H)-quinazolinedione ([(11)C]KF21652) and examined its potential as a positron emission tomography (PET) ligand for mapping adenosine transporters in the brain and peripheral organs. The log P(7.4) value of KF21652 was 3.14, and the K(i) value was 13 nM for adenosine transporters using [(3)H]nitrobenzylthioinosine as a radioligand. In mice, the highest initial uptake was found in the liver, followed by the kidney and small intestine. The brain uptake was very low. The radioactivity level slightly increased with time in the liver and small intestine, but decreased in the other organs. Coinjection of carrier KF21652 slightly decreased the uptake of [(11)C]KF21562 only in the liver, but not in any other organs. Ex vivo autoradiography of the rat brain showed that [(11)C]KF21652 was scarcely incorporated into the brain. On the other hand, in vitro autoradiography showed the binding of [(11)C]KF21562 to adenosine transporters with high nonspecific binding. These results show that the compound is not a suitable PET ligand for mapping adenosine transporters.
    Nuclear Medicine and Biology 05/2001; 28(3):281-5. DOI:10.1016/S0969-8051(00)00170-0 · 2.41 Impact Factor
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    ABSTRACT: In vivo assessment of the adenosine A(2A) receptors localized in the striatum with positron emission tomography (PET) may offers us a new diagnostic tool for neurological disorders. We evaluated the potential of [7-methyl-(11)C](E)-8-(2,3-dimethyl-4-methoxystyryl)-1, 3,7-trimethylxanthine ([(11)C]KF21213) as a PET ligand for mapping adenosine A(2A) receptors in the central nervous system. KF21213 showed a high affinity for the adenosine A(2A) receptors in vitro (Ki = 3.0 nM) and a very low affinity for the A(1) receptors (Ki > 10,000 nM). In mice, the striatal uptake of [(11)C]KF21213 increased for the first 15 min and then gradually decreased, whereas the uptake in the reference regions such as the cortex and cerebellum rapidly decreased. The uptake ratio of striatum to cortex and striatum to cerebellum increased to 8.6 and 10.5, respectively, at 60 min postinjection. The striatal uptake was significantly blocked by co-injection of carrier KF21213 or each of three other A(2A) antagonists, but not by co-injection of A(1) antagonist. The specific uptake was not detected in the cortex or in the cerebellum. Ex vivo autoradiography and PET clearly visualized adenosine A(2A) receptors in the rat striatum. [(11)C]KF21213 was the most selective tracer for mapping adenosine A(2A) in the central nervous system by PET among the tracers proposed to date.
    Nuclear Medicine and Biology 09/2000; 27(6):541-6. DOI:10.1016/S0969-8051(00)00126-8 · 2.41 Impact Factor
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    ABSTRACT: The potential of the (11)C-labeled selective sigma(1) receptor ligand 1-(3,4-dimethoxyphenethyl)-4-(3-phenylpropyl)piperazine ([(11)C]SA4503) was evaluated in vivo as a positron emission tomography (PET) ligand for mapping sigma(1) receptors in rats. SA4503 is known to have a high affinity (IC(50) = 17.4 nM) and a higher selectivity (sigma(1)/sigma(2) = 103) for the sigma(1) receptor. A high and increasing brain uptake of [(11)C]SA4503 was found. Pre-, co- and postinjection of cold SA4503 significantly decreased uptake of [(11)C]SA4503 in the brain, spleen, heart, lung, and kidney in which sigma receptors are present as well as in the skeletal muscle. In the blocking study with one of four sigma receptor ligands including haloperidol, (+)-pentazocine, SA4503, and (-)-pentazocine (in the order of their affinity for sigma(1) receptor subtype), SA4503 and haloperidol significantly reduced the brain uptake of [(11)C]SA4503 to approximately 30% of the control, but the other two benzomorphans did not. A high specific uptake of [(11)C]SA4503 by the brain was also confirmed by ex vivo autoradiography (ARG) and PET. Ex vivo ARG showed a higher uptake in the vestibular nucleus, temporal cortex, cingulate cortex, inferior colliculus, thalamus, and frontal cortex, and a moderate uptake in the parietal cortex and caudate putamen. Peripherally, the blocking effects of the four ligands depended on their affinity for sigma(1) receptors. No (11)C-labeled metabolite was detected in the brain 30 min postinjection, whereas approximately 20% of the radioactivity was found as (11)C-labeled metabolites in plasma. These results have demonstrated that the (11)C-labeled sigma(1) receptor ligand [(11)C]SA4503 has a potential for mapping sigma(1) receptors in the central nervous system and peripheral organs.
    Nuclear Medicine and Biology 05/2000; 27(3):255-61. DOI:10.1016/S0969-8051(00)00081-0 · 2.41 Impact Factor
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    ABSTRACT: The present investigation was undertaken to identify the long-lived radionuclide and its chemical forms existing in [15O]water which was synthesized from 15O produced by the nuclear reaction 14N(d,n)15O, and to develop a method for its removal to facilitate radioactive waste disposal. The long-lived nuclide was identified as tritium based on a comparison of its physical half-life and the energy spectrum of β-rays with those of tritium. The major chemical form of tritium in the target gas was estimated to be molecular hydrogen. The tritium radioactivity was completely removed without a serious loss occurring to the yield of [15O]water by passing the irradiated target gas over a heated palladium catalyst followed by a calcium chloride column before the final synthesis of the [15O]water. This provided a practical way of removing tritium from the [15O]water.
    Applied Radiation and Isotopes 03/2000; 52(2):175-179. DOI:10.1016/S0969-8043(99)00134-7 · 1.06 Impact Factor
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    ABSTRACT: HPLC separation of either [11C]β-CFT or [11C]β-CIT from the N-desmethyl precursor greatly depended on the ODS column used and the pH of the phosphate buffer in the mobile phase. The separation was accomplished on the semipreparative reversed phase ODS column without end-capping treatment over a pH ranging from 6.4 to 9.2, but failed on the end-capped ODS column. This suggests that the presence of residual silanol groups on the ODS is an important factor for the separation.
    Applied Radiation and Isotopes 03/2000; DOI:10.1016/S0969-8043(99)00152-9 · 1.06 Impact Factor
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    ABSTRACT: The potential of a 11C-labeled selective sigma1 receptor ligand, 1-(3,4-dimethoxyphenethyl)-4-[3-(3,4-dichlorophenyl)propyl]piperazine ([11C]SA6298), was evaluated as a positron emission tomography (PET) ligand for mapping sigma, receptors in the central nervous system and peripheral organs. [11C]SA6298 was synthesized by methylation of the desmethyl SA6298 with [11C]CH3I, with the decay-corrected radiochemical yield of 39 +/- 5% based on [11C]CH3I and with the specific activity of 53 +/- 17 TBq/mmol within 20 min from end of bombardment (EOB). In mice, the uptake of [11C]SA6298 was significantly decreased by carrier loading in the brain, liver, spleen, heart, lung, small intestine, and kidney in which sigma receptors are present as well as in the skeletal muscle. Pretreatment with SA6298 also blocked the uptake of [11C]SA6298 by these organs except for the small intestine, but significant displacement of [11C]SA6298 by posttreatment with SA6298 was observed only in the heart, lung, and muscle. In the blocking study with one of the eight sigma receptor ligands, including haloperidol, SA6298, NE-100, (+)-pentazocine, SA4503, (-)-pentazocine, (+)-3-PPP, and (+)-SKF 10,047 (in the order of the affinity for sigma1 receptor subtype), only SA6298 and an analog SA4503 significantly reduced the brain uptake of [11C]SA6298 to approximately 80% of the control, but the other six ligands did not. Peripherally, the uptake of [11C]SA6298 by the organs described above was decreased predominantly by SA6298 or SA4503, but the blocking effects of the other five ligands except for NE-100 depended on their affinity for sigma1 receptors. The saturable brain uptake of [11C]SA6298, approximately 20%, was also observed by tissue dissection method in rats and by PET in a cat. Ex vivo autoradiography of the rat brain showed a high uptake in the cortex and thalamus. In the cat brain a relatively high uptake was found in the cortex, thalamus, striatum, and cerebellum. These results have indicated a receptor-mediated uptake of the tracer to some extent in the brain and peripheral organs. However, the tracer has a limited potential for the PET study of the brain receptors because of a relatively high nonspecific binding.
    Nuclear Medicine and Biology 12/1999; 26(8):915-22. DOI:10.1016/S0969-8051(99)00069-4 · 2.41 Impact Factor
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    ABSTRACT: No carrier added (nca) 2-amino-4-([11C]methylthio) butyric acid ([11C]methionine, [11C]MET) was prepared by the reaction of O-acetyl-l-homoserine and [11C]methanethiol using immobilized γ-cyano-α-aminobutylic acid synthase. If one passed [11C]methyl iodide through a DMF solution containing NaSH at 120°C, approximately 90% of the radioactivity was converted to [11C]methanethiol with the radiochemical purity of >99%, which was trapped in acetone cooled at −30 to −50°C. After the buffer containing a substrate for the enzyme reaction was added, the aqueous acetone solution was passed through a small column packed with the immobilized enzyme (6.0 mm i.d.×17 mm length) at room temperature for approximately 1 min. Approximately 80% of [11C]methanethiol applied to the column was recovered as only [11C]MET. After dryness was achieved in vacuo, the residue was dissolved in physiological saline and the solution was passed through a membrane filter. The radiochemically and enatiomerically pure [11C]MET was ready for injection within 15 min after the end of irradiation. [11C]MET analogues such as [11C]ethionine and [11C]propionine were also prepared from corresponding [11C]alkanethiols.
    Applied Radiation and Isotopes 09/1999; 51(3-51):285-291. DOI:10.1016/S0969-8043(98)00198-5 · 1.06 Impact Factor
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    ABSTRACT: We have developed a novel autoradiographic method of visualizing oxygen fixation with sufficient delivery of []O2/O2. Brain slices (400 μm) were preincubated in Krebs–Ringer phosphate buffer and exposed to []O2 in a chamber. Fixation of []O2 correlated with the polarographically measured oxygen consumption among tissue slices from various organs (r=0.84). The fixation of []O2 by brain slices was significantly reduced (7.2% of the control) by heat-treatment or dose dependently by NaCN (18.2% of the control on 50 mM NaCN pretreatment). The radioactivity in the brain slices prepared from rotenone injected rats was also reduced compared to the control (56.8% of the control side). In an autoradiographic study, radioactivity showed a heterogeneous distribution both in coronal and sagittal sections. Autoradiography of young and senescent rat brain sections showed reduction of oxygen uptake with aging in the cerebrum, the senescent being 77.4% of the young. This method provides information regarding basic oxygen consumption of tissue slices under condition of sufficient O2 delivery, which reflects mitochondrial electron transport.
    Brain Research 07/1999; 831(1-2-831):263-272. DOI:10.1016/S0006-8993(99)01464-X · 2.83 Impact Factor
  • Kiichi Ishiwata, Shin-ichi Ishii, Michio Senda
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    ABSTRACT: The standard method of [11C]raclopride synthesis requires a large amount of its desmethyl precursor. We prepared [11C]raclopride by methylation of a small amount of desmethyl derivative (0.3-0.5 mg) with [11C]methyl iodide in a DMF solution containing NaH, with a decay-corrected radiochemical yield of 11-14% based on [11C]methyl iodide and with a specific activity of 48 TBq/mmol for 25 min from EOB. The reaction was reproducible and reliable.
    Annals of Nuclear Medicine 07/1999; 13(3):195-7. DOI:10.1007/BF03164862 · 1.51 Impact Factor
  • Toru Sasaki, Koji Ogawa, Shin-Ichi Ishii, Michio Senda
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    ABSTRACT: For in vivo measurement of the hydroxyl radical (.OH), we synthesized [11C]salicylic acid, [11C]O-acetylsalicylic acid and [11C]2-methoxybenzoic acid by carboxylation of 2-bromomagnesiumanisol using [11C]CO2. The radiochemical yield of [11C]salicylic acid, [11C]O-acetylsalicylic acid and [11C]2-methoxybenzoic acid calculated from trapped [11C]CO2 in a liquid argon cooled stainless tube was 7.3 +/- 1.6, 5.2 and 10.2 +/- 1.7% (decay corrected), respectively. The uptake of 11C tracers by mouse brain was 0.46, 0.32, and 0.46% dose/g tissue, respectively, at 10 min post injection and presented washout patterns thereafter.
    Applied Radiation and Isotopes 06/1999; 50(5):905-9. DOI:10.1016/S0969-8043(98)00144-4 · 1.06 Impact Factor
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    ABSTRACT: Carbon-11 labeled alkyl iodides such as ethyl, propyl and butyl iodides are useful precursors for labeling various tracers for positron emission tomography. In the standard preparing process, which consists of the reaction of Grignard reagents with 11CO2 followed by reduction with lithium aluminum hydride and reaction with HI, the produced 11C-alkyl iodides were applied onto gas chromatography using chromosorb W-HP with 10% OV101 as the liquid phase, to give radiochemically pure 11C-ethyl, 11C-propyl or 11C-butyl iodide without a concomitant byproduct, i.e. 11C-methyl iodide. The automated production system was described.
    Applied Radiation and Isotopes 04/1999; 50(4):693-697. DOI:10.1016/S0969-8043(98)00090-6 · 1.06 Impact Factor
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    ABSTRACT: We have studied the synthesis of [11C]2,3-dimethoxy-5-methyl-6-(10-hydroxy)-decyl-1,4-benzoquinone (idebenone) and [11C]2,3-dimethoxy-5-methyl-1,4-benzoquinone (CoQo) by methylation of their respective desmethyl precursors using [11C]CH3I for in vivo measurement of mitochondrial electron transfer and redox state. The [11C]idebenone was more lipophilic than [11C]CoQo; the latter became hydrophilic by reduction. Clearance of [11C]idebenone from mouse brain was more rapid than that of [11C]CoQo. The results indicated that modification of the isoprenoid side chain in [11C]CoQ is necessary to develop more suitable radiopharmaceuticals.
    Nuclear Medicine and Biology 03/1999; 26(2):183-7. DOI:10.1016/S0969-8051(98)00096-1 · 2.41 Impact Factor
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    ABSTRACT: N,N-Dipropyl-2-[4-methoxy-3-(2-phenylethoxy)phenyl]ethylamine (NE-100) was labeled with 11C in two different positions by the alkylation of an N-despropyl precursor with [11C]propyl iodide and of an O-desmethyl precursor with [11C]methyl iodide and was evaluated for the potential as a tracer for mapping σ 1 receptors in the CNS and peripheral organs by PET. Following i.v. injection of [N-propyl-11C]NE-100 or [O-methyl-11C]NE-100 into mice, the two tracers showed similar tissue distribution patterns except for the liver and brain. With the coinjected carrier NE-100 or haloperidol, the uptake of [N-propyl-11C]NE-100 by the liver, pancreas and spleen was significantly decreased at 15 min after injection, whereas the effect was not significant for [O-methyl-11C]NE-100. The coinjection of NE-100 enhanced the brain uptake of the two tracers. Haloperidol also enhanced the brain uptake of [N-propyl-11C]NE-100, but not that of [O-methyl-11C]NE-100. The regional brain distribution assessed with [O-methyl-3H]NE-100 was consistent with the distribution pattern of the σ receptors. Four σ drugs reduced the regional brain uptake of [O-methyl-3H]NE-100 to 70%–90% of the control. In an ex vivo autoradiographic study of the rat brain, the uptake of [O-methyl-11C]NE-100 was blocked by carrier NE-100 or haloperidol (53%–59% of the control in the cortex), which suggests a receptor-specific distribution. These results show that [O-methyl-11C]NE-100 has limited potential as a PET ligand for mapping σ 1 receptors in the peripheral organs and the CNS because of high nonspecific binding.
    Nuclear Medicine and Biology 04/1998; 25(3):195-202. DOI:10.1016/S0969-8051(97)00170-4 · 2.41 Impact Factor
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    ABSTRACT: In the neuronal activation study of normal animals, precise anatomical correlation, preferentially to a detailed brain atlas, is required for the activation foci co-registration. To obtain precise regional correlation between H(2)15O-PET images and the brain atlas, a method of stereotaxic image reorientation was applied to an activation study with vibrotactile stimulation. Cats anesthetized with halothane underwent repeated measurements of regional cerebral blood flow (rCBF) in the resting condition and during vibration of the right forepaw. The image set was adjusted three-dimensionally to the atlas. The postmortem brain was sectioned according to the atlas planes. The activated areas were determined by the stimulus-minus-resting subtraction images, and the areas were projected to the atlas. The PET images of the cat brain were compatible both to the postmortem brain slices and to the brain atlas. The activation foci obtained from the subtraction images corresponded to the area around the coronal sulcus, which is electrophysiologically known as the primary sensory area as described in the atlas. There were precise regional correlations between the PET image and anatomy in a PET activation study of the cat by means of stereotaxic image reorientation.
    Annals of Nuclear Medicine 12/1997; 11(4):315-9. DOI:10.1007/BF03165299 · 1.51 Impact Factor
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    ABSTRACT: To develop 18F-fluoroalkyl derivatives of methionine (MET) as a tumor detecting agent by mean of clinical PET, a pilot study assessing the potential of their parent compounds, 11C-labeled ethionine (11C-ETH) and propionine (11C-PRO), was performed. 11C-ETH and 11C-PRO were prepared by the reaction of L-homocysteine thiolactone and corresponding 11C-alkyl iodides. After i.v. injection of a mixture of 3H-MET. 14C-ETH and 11C-PRO into mice bearing FM3A mammary carcinoma, the highest FM3A uptake was found in 14C-ETH, followed by 3H-MET and 11C-PRO, while the FM3A-to-brain and FM3A-to-muscle ratios were nearly the same for all three compounds. The FM3A uptake of 14C-ETH and 11C-PRO were nearly equal or slightly higher than the liver uptake. In the pancreas, liver, FM3A and brain tissues, incorporation of 14C-ETH into acid-precipitable materials was much lower than that of 3H-MET, whereas no incorporation of 11C-PRO was found. Brain uptake of all three compounds was significantly reduced by carrier MET-loading (5 min p.i.) or by cycloheximide treatment to inhibit protein synthesis (60 min p.i.), whereas the FM3A uptake was not affected. Incorporation of 14C-ETH into acid-precipitable materials was inhibited by the cycloheximide. The results suggest that 11C-labeled ETH has a similar potential for tumor detection by PET as 11C-MET, and that 11C-PRO has similar properties to those of other artificial amino acids. The development of 18F-fluoroalkyl derivatives of MET is of interest as the next step.
    Annals of Nuclear Medicine 06/1997; 11(2):115-22. DOI:10.1007/BF03164819 · 1.51 Impact Factor
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    ABSTRACT: We prepared [11C]KF15372 ([1-propyl-11C]8-dicyclopropylmethyl-1,3-dipropylxanthine, refs 10, 13) as well as its 11C-ethyl and 11C-methyl derivatives ([11C]EPDX and [11C]MPDX), and examined the potential of the three compounds as PET ligands for CNS adenosine A1 receptors. The three compounds had high affinity for the A1 receptors in vitro in the following order; [11C]EPDX > [11C]KF15372 > [11C]MPDX. In mice, the highest initial brain uptake was found in [11C]MPDX followed by [11C]EPDX and [11C]KF15372, but the level of [11C]MPDX decreased faster than those of the other two compounds. The uptake of each compound was decreased by carrier KF15372, but not by an A2A antagonist, indicating the selective affinity for the A1 receptors. Autoradiography with [11C]MPDX ex vivo demonstrated decreased A1 receptor binding in the superior colliculus of rats deprived of retino-collicular fibers by contralateral eye enucleation. These results show that three compounds have potential as PET ligands for CNS adenosine A1 receptors.
    Nuclear Medicine and Biology 02/1997; 24(1):53-9. DOI:10.1016/S0969-8051(96)00161-8 · 2.41 Impact Factor
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    ABSTRACT: Positron emission tomography (PET) was performed on the cat brain to characterize [1-11C]hexanoate and other [1-11C]labeled short and medium-chain fatty acids as a tracer of fatty acid oxidative metabolism. After an intravenous injection the brain uptake of [1-11C]hexanoate reached a peak followed by rapid washout until 2 min (first phase). Subsequently the total brain uptake was again increased and reached to a peak 7-10 min after tracer injection (second phase). The blood radioactivity of unmetabolized [1-11C]hexanoate was rapidly decreased and almost eliminated within the first 2 min, whereas the blood radioactivity of [11C]CO2/HCO3- was gradually increased and reached a peak approximately 5 min after tracer injection. As the effect of circulating [11C]CO2/HCO3- was examined by a bolus intravenous injection of [11C]CO2/HCO3-, the brain uptake of [11C]CO2/HCO3- was rapidly increased right after the injection and changed parallel to the blood level of [11C]CO2/HCO3-. These results suggest that, in contrast to the previous mouse data, the time-activity curve in the cat brain following intravenous injection of [1-11C]hexanoate has a biphasic pattern, the second phase being determined by peripherally originating [11C]CO2/HCO3-, and therefore does not reflect the metabolism of 11C-labeled fatty acid in the brain.
    Annals of Nuclear Medicine 09/1996; 10(3):361-6. DOI:10.1007/BF03164748 · 1.51 Impact Factor
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    ABSTRACT: In the quantitative studies of presynaptic dopamine metabolism by PET with 6-[18F]fluoro-L-dopa (6-[18F]FDOPA), metabolic analysis in the plasma is required to determine the precise input function because of susceptibility of the compound to peripheral metabolism. In this study, we prepared 6-[18F]-fluoro-O-pivaloyl-L-dopa (6-[18F]FPDOPA) as a prodrug of 6-[18F]FDOPA, and evaluated its potential as a PET tracer in mice. If the 6-[18F]FPDOPA is stable peripherally and is hydrolyzed to 6-[18F]FDOPA in the brain tissues, disadvantage of the 6-[18F]FDOPA will be overcome. Compared with the 6-[18F]FDOPA, the initial brain uptake of the 6-[18F]FPDOPA was lower; however, the uptake in the latter become comparable, and the uptake ratios of striatum to other reference regions were larger. Medication of mice with inhibitors of aromatic amino acid decarboxylase and catechol-O-methyl transferase greatly enhanced the striatal uptake of the two compounds. The reduced brain uptake of the compounds by L-phenylalanine-loading suggested transport through the blood-brain barrier by the neutral amino acid transporter. HPLC analysis showed the presence of 6-[18F]FPDOPA, 6-[18F]FDOPA and 6-[18F]fluorodopamine in the striatum; however, 6-[18F]fluoro-3-O-methyl-L-dopa was a predominate metabolite in the brain and plasma as in the case of [18F]FDOPA. Results suggested that 6-[18F]FPDOPA had characteristics as a prodrug of 6-[18F]FDOPA; however, the compound was also labile to metabolic alteration in vivo.
    Nuclear Medicine and Biology 05/1996; 23(3):295-301. DOI:10.1016/0969-8051(95)02083-7 · 2.41 Impact Factor
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    ABSTRACT: An 11C-labeled selective adenosine A2A antagonist, (E)-8-(3,4-dimethoxystyryl)-1,3-dipropyl-7-[11C]-methylxanthine ([11C]KF17837), was prepared by reaction of (E)-8-(3,4-dimethoxystyryl)-1,3-dipropylxanthine and [11C]methyl iodide with decay-corrected radiochemical yield of 19-50%, radiochemical purity of > 99%, sp. act. of 17-100 GBq/mumol and preparation time of 20-25 min. In mice, the myocardium showed the highest (13.4% ID/g) at 5 min after i.v. injection, which decreased gradually with time. The specific myocardial uptake was visualized by gamma-camera. In the brain region the radioactivity level was higher in the A2A receptors-rich striatum than in the cortex and cerebellum. The specific striatal uptake in rats was clearly demonstrated by PET. These results have shown that [11C]KF17837 is a potential PET radioligand for mapping the adenosine A2A receptors in the heart and brain.
    Applied Radiation and Isotopes 05/1996; 47(5-6):507-11. DOI:10.1016/0969-8043(95)00295-2 · 1.06 Impact Factor