Takahiro Mukai

Summary

Affiliation: Kyushu University
Country: Japan

Publications

  1. ncbi request reprint Synthesis of a beta-tetrapeptide analog as a mother compound for the development of matrix metalloproteinase-2-imaging agents
    Takahiro Mukai
    Graduate School of Pharmaceutical Sciences, Kyushu University, 3 1 1 Maidashi, Higashi ku, Fukuoka 812 8582, Japan
    Chem Pharm Bull (Tokyo) 56:260-5. 2008
  2. ncbi request reprint [Development of bifunctional radiopharmaceuticals for targeted imaging and therapy]
    Takahiro Mukai
    Faculty of Pharmaceutical Sciences, Kyushu University, 3 1 1 Maidashi, Higashi ku, Fukuoka 812 8582, Japan
    Yakugaku Zasshi 127:1937-45. 2007
  3. doi request reprint Design of Ga-DOTA-based bifunctional radiopharmaceuticals: two functional moieties can be conjugated to radiogallium-DOTA without reducing the complex stability
    Takahiro Mukai
    Department of Biomolecular Recognition Chemistry, Graduate School of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan
    Bioorg Med Chem 17:4285-9. 2009
  4. doi request reprint Development of N-[11C]methylamino 4-hydroxy-2(1H)-quinolone derivatives as PET radioligands for the glycine-binding site of NMDA receptors
    Takeshi Fuchigami
    Graduate School of Pharmaceutical Sciences, Kyushu University, Higashi ku, Fukuoka 812 8582, Japan
    Bioorg Med Chem 17:5665-75. 2009
  5. ncbi request reprint Radiosynthesis and biodistribution in mice of a 18F-labeled analog of O-1302 for use in cerebral CB1 cannabinoid receptor imaging
    Yumiko Nojiri
    Graduate School of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan
    Biol Pharm Bull 31:1274-8. 2008
  6. ncbi request reprint Chemical design of a radiolabeled gelatinase inhibitor peptide for the imaging of gelatinase activity in tumors
    Hirofumi Hanaoka
    Graduate School of Pharmaceutical Sciences, Kyoto University, Yoshida Shimoadachi cho, Kyoto 606 8501, Japan
    Nucl Med Biol 34:503-10. 2007
  7. doi request reprint Usefulness of competitive inhibitors of protein binding for improving the pharmacokinetics of 186Re-MAG3-conjugated bisphosphonate (186Re-MAG3-HBP), an agent for treatment of painful bone metastases
    Kazuma Ogawa
    Department of Patho Functional Bioanalysis, Graduate School of Pharmaceutical Sciences, Kyoto University, Yoshida Shimoadachi cho, Sakyo ku, Kyoto, 606 8501, Japan
    Eur J Nucl Med Mol Imaging 36:115-21. 2009
  8. ncbi request reprint Development of a 111In-labeled peptide derivative targeting a chemokine receptor, CXCR4, for imaging tumors
    Hirofumi Hanaoka
    Graduate School of Pharmaceutical Sciences, Kyoto University, Yoshida Shimoadachi cho, Sakyo ku, Kyoto 606 8501, Japan
    Nucl Med Biol 33:489-94. 2006
  9. ncbi request reprint In vitro system to estimate renal brush border enzyme-mediated cleavage of Peptide linkages for designing radiolabeled antibody fragments of low renal radioactivity levels
    Yasushi Fujioka
    Graduate School of Pharmaceutical Sciences, Kyoto University, Japan
    Bioconjug Chem 16:1610-6. 2005
  10. ncbi request reprint Rhemium-186-monoaminemonoamidedithiol-conjugated bisphosphonate derivatives for bone pain palliation
    Kazuma Ogawa
    Graduate School of Pharmaceutical Sciences, Kyoto University, Yoshida Shimoadachi cho, Sakyo ku, Kyoto 606 8501, Japan
    Nucl Med Biol 33:513-20. 2006

Collaborators

Detail Information

Publications62

  1. ncbi request reprint Synthesis of a beta-tetrapeptide analog as a mother compound for the development of matrix metalloproteinase-2-imaging agents
    Takahiro Mukai
    Graduate School of Pharmaceutical Sciences, Kyushu University, 3 1 1 Maidashi, Higashi ku, Fukuoka 812 8582, Japan
    Chem Pharm Bull (Tokyo) 56:260-5. 2008
    ..These findings suggest that compound 1 may serve as a mother compound in the design and development of in vivo MMP-2-imaging agents...
  2. ncbi request reprint [Development of bifunctional radiopharmaceuticals for targeted imaging and therapy]
    Takahiro Mukai
    Faculty of Pharmaceutical Sciences, Kyushu University, 3 1 1 Maidashi, Higashi ku, Fukuoka 812 8582, Japan
    Yakugaku Zasshi 127:1937-45. 2007
    ..This review summarizes our examples of chemical design of in vivo radiopharmaceuticals to achieve the targeted imaging and therapy...
  3. doi request reprint Design of Ga-DOTA-based bifunctional radiopharmaceuticals: two functional moieties can be conjugated to radiogallium-DOTA without reducing the complex stability
    Takahiro Mukai
    Department of Biomolecular Recognition Chemistry, Graduate School of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan
    Bioorg Med Chem 17:4285-9. 2009
    ..These results indicate the potential benefits of the drug design of (67)Ga-DOTA-MN2. The present findings provide helpful information for the development of radiogallium-labeled radiopharmaceuticals for SPECT and PET studies...
  4. doi request reprint Development of N-[11C]methylamino 4-hydroxy-2(1H)-quinolone derivatives as PET radioligands for the glycine-binding site of NMDA receptors
    Takeshi Fuchigami
    Graduate School of Pharmaceutical Sciences, Kyushu University, Higashi ku, Fukuoka 812 8582, Japan
    Bioorg Med Chem 17:5665-75. 2009
    ..It is conjectured that still acidic moiety and high affinity with plasma protein of [(11)C]32 may prevent in vivo brain uptake. In conclusion, [(11)C]12 and [(11)C]32 are unsuitable for imaging cerebral NMDA receptors...
  5. ncbi request reprint Radiosynthesis and biodistribution in mice of a 18F-labeled analog of O-1302 for use in cerebral CB1 cannabinoid receptor imaging
    Yumiko Nojiri
    Graduate School of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan
    Biol Pharm Bull 31:1274-8. 2008
    ..Radioligand [18F]1 does not have the required properties for imaging the cerebral cannabinoid CB1 receptor in vivo...
  6. ncbi request reprint Chemical design of a radiolabeled gelatinase inhibitor peptide for the imaging of gelatinase activity in tumors
    Hirofumi Hanaoka
    Graduate School of Pharmaceutical Sciences, Kyoto University, Yoshida Shimoadachi cho, Kyoto 606 8501, Japan
    Nucl Med Biol 34:503-10. 2007
    ..Furthermore, (111)In-DTPA-CTT derivatives would be potential radiopharmaceuticals for the imaging of gelatinase activity in metastatic tumors in vivo...
  7. doi request reprint Usefulness of competitive inhibitors of protein binding for improving the pharmacokinetics of 186Re-MAG3-conjugated bisphosphonate (186Re-MAG3-HBP), an agent for treatment of painful bone metastases
    Kazuma Ogawa
    Department of Patho Functional Bioanalysis, Graduate School of Pharmaceutical Sciences, Kyoto University, Yoshida Shimoadachi cho, Sakyo ku, Kyoto, 606 8501, Japan
    Eur J Nucl Med Mol Imaging 36:115-21. 2009
    ....
  8. ncbi request reprint Development of a 111In-labeled peptide derivative targeting a chemokine receptor, CXCR4, for imaging tumors
    Hirofumi Hanaoka
    Graduate School of Pharmaceutical Sciences, Kyoto University, Yoshida Shimoadachi cho, Sakyo ku, Kyoto 606 8501, Japan
    Nucl Med Biol 33:489-94. 2006
    ..These findings suggested that 111In-DTPA-Ac-TZ14011 would be a potential agent for the imaging of CXCR4 expression in metastatic tumors in vivo...
  9. ncbi request reprint In vitro system to estimate renal brush border enzyme-mediated cleavage of Peptide linkages for designing radiolabeled antibody fragments of low renal radioactivity levels
    Yasushi Fujioka
    Graduate School of Pharmaceutical Sciences, Kyoto University, Japan
    Bioconjug Chem 16:1610-6. 2005
    ..This study suggested that this in vitro system using BBMVs would be useful to estimate radiolabeling reagents of antibody fragments or peptides designed to reduce renal radioactivity with a variety of radionuclides...
  10. ncbi request reprint Rhemium-186-monoaminemonoamidedithiol-conjugated bisphosphonate derivatives for bone pain palliation
    Kazuma Ogawa
    Graduate School of Pharmaceutical Sciences, Kyoto University, Yoshida Shimoadachi cho, Sakyo ku, Kyoto 606 8501, Japan
    Nucl Med Biol 33:513-20. 2006
    ..These findings provide useful information on the design of bone-seeking therapeutic radiopharmaceuticals...
  11. ncbi request reprint 5-[123I]Iodo-A-85380: assessment of pharmacological safety, radiation dosimetry and SPECT imaging of brain nicotinic receptors in healthy human subjects
    Masashi Ueda
    Department of Patho Functional Bioanalysis, Graduate School of Pharmaceutical Sciences, Kyoto University, Japan
    Ann Nucl Med 18:337-44. 2004
    ..These results suggest that [123I]5IA is a promising ligand for imaging nAChRs in humans, with an acceptable dosimetry and pharmacological safety at the dose required for adequate SPECT imaging...
  12. doi request reprint Targeting of lectinlike oxidized low-density lipoprotein receptor 1 (LOX-1) with 99mTc-labeled anti-LOX-1 antibody: potential agent for imaging of vulnerable plaque
    Seigo Ishino
    Department of Patho Functional Bioanalysis, Graduate School of Pharmaceutical Sciences, Kyoto University, Kyoto, Japan
    J Nucl Med 49:1677-85. 2008
    ..In this study, we designed and prepared (99m)Tc-labeled anti-LOX-1 monoclonal IgG and investigated its usefulness as an atherosclerosis imaging agent...
  13. ncbi request reprint Evaluation of 5-(11)C-methyl-A-85380 as an imaging agent for PET investigations of brain nicotinic acetylcholine receptors
    Yasuhiko Iida
    Department of Patho Functional Bioanalysis, Graduate School of Pharmaceutical Sciences, Kyoto University, Kyoto, Japan
    J Nucl Med 45:878-84. 2004
    ....
  14. ncbi request reprint Development of a novel 99mTc-chelate-conjugated bisphosphonate with high affinity for bone as a bone scintigraphic agent
    Kazuma Ogawa
    Department of Patho Functional Bioanalysis, Graduate School of Pharmaceutical Sciences, Kyoto University, Kyoto, Japan
    J Nucl Med 47:2042-7. 2006
    ....
  15. ncbi request reprint 5-O-(4-[125 I]Iodobenzyl)-L-ascorbic acid: electrophilic radioiodination and biodistribution in mice
    Jintaek Kim
    Graduate School of Pharmaceutical Sciences, Kyushu University, 3 1 1 Maidashi, Higashi ku, Fukuoka, Japan
    Chem Pharm Bull (Tokyo) 60:235-40. 2012
    ..Introduction of a bulky substituent at C-5 on AsA, such as an iodobenzyloxy group, may not be suitable for the design of analogs that may still be able to maintain characteristic distribution properties in vivo seen with AsA itself...
  16. doi request reprint PET imaging of hypoxia-inducible factor-1-active tumor cells with pretargeted oxygen-dependent degradable streptavidin and a novel 18F-labeled biotin derivative
    Takashi Kudo
    Department of Patho Functional Bioanalysis, Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo ku, Kyoto, Japan
    Mol Imaging Biol 13:1003-10. 2011
    ..We aimed to evaluate the feasibility of using streptavidin-biotin-based pretargeting for positron emission tomography (PET) imaging of hypoxia-inducible factor (HIF)-1-active tumors...
  17. ncbi request reprint Therapeutic effects of a 186Re-complex-conjugated bisphosphonate for the palliation of metastatic bone pain in an animal model
    Kazuma Ogawa
    Department of Patho Functional Bioanalysis, Graduate School of Pharmaceutical Sciences, Kyoto University, Kyoto, Japan
    J Nucl Med 48:122-7. 2007
    ..In this study, we evaluated the therapeutic effects of (186)Re-MAG3-HBP using an animal model of bone metastasis...
  18. ncbi request reprint ¹¹C-labeled analogs of indomethacin esters and amides for brain cyclooxygenase-2 imaging: radiosynthesis, in vitro evaluation and in vivo characteristics in mice
    Yumi Yamamoto
    Graduate School of Pharmaceutical Sciences, Kyushu University, Japan
    Chem Pharm Bull (Tokyo) 59:938-46. 2011
    ..Further structural refinement of the tracer agent is necessary for better enhancement of brain uptake and for sufficient metabolic stability...
  19. doi request reprint Imaging of HIF-1-active tumor hypoxia using a protein effectively delivered to and specifically stabilized in HIF-1-active tumor cells
    Takashi Kudo
    Department of Patho Functional Bioanalysis, Graduate School of Pharmaceutical Sciences, Kyoto University, Kyoto, Japan
    J Nucl Med 50:942-9. 2009
    ..The purpose of this study was to evaluate the feasibility of (123)I-IPOS as an imaging probe for HIF-1-active tumor hypoxia...
  20. ncbi request reprint Development of a rhenium-186-labeled MAG3-conjugated bisphosphonate for the palliation of metastatic bone pain based on the concept of bifunctional radiopharmaceuticals
    Kazuma Ogawa
    Department of Patho Functional Bioanalysis, Graduate School of Pharmaceutical Sciences, Kyoto University, Yoshida Shimoadachi cho, Sakyo ku, Kyoto 606 8501, Japan
    Bioconjug Chem 16:751-7. 2005
    ..In addition, the gastric accumulation of 186Re-MAG3-HBP radioactivity was lower than that of 186Re-HEDP. In conclusion, 186Re-MAG3-HBP is expected to be a useful radiopharmaceutical for the palliation of metastatic bone pain...
  21. ncbi request reprint Radiosynthesis and evaluation of 11C-labeled diaryl-substituted imidazole and indole derivatives for mapping cyclooxygenase-2
    Mariko Tanaka
    Graduate School of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan
    Biol Pharm Bull 29:2087-94. 2006
    ..There seem to be some obstacles to finding a useful candidate for in vivo imaging application of COX-2 selective inhibitors only by standard consideration of in vitro affinity and selectivity, and the lipophilicity of the compound...
  22. ncbi request reprint Prominent lectin-like oxidized low density lipoprotein (LDL) receptor-1 (LOX-1) expression in atherosclerotic lesions is associated with tissue factor expression and apoptosis in hypercholesterolemic rabbits
    Yuji Kuge
    Department of Patho Functional Bioanalysis, Graduate School of Pharmaceutical Sciences, Kyoto University, Kyoto, Japan
    Biol Pharm Bull 31:1475-82. 2008
    ..Here, we compared the in vivo expression of LOX-1, with tissue factor (TF) expression and cell apoptosis, in atherosclerotic lesions of myocardial infarction-prone Watanabe heritable hyperlipidemic (WHHLMI) rabbits...
  23. ncbi request reprint In vivo evaluation of a radiogallium-labeled bifunctional radiopharmaceutical, Ga-DOTA-MN2, for hypoxic tumor imaging
    Kohei Sano
    Department of Biomolecular Recognition Chemistry, Graduate School of Pharmaceutical Sciences, Kyushu University, 3 1 1 Maidashi, Fukuoka 812 8582, Japan
    Biol Pharm Bull 36:602-8. 2013
    ..The present findings provide useful information about the chemical design of radiogallium-labeled radiopharmaceuticals for PET and single photon emission computed tomography (SPECT) studies...
  24. ncbi request reprint 6-Deoxy-6-[131I]iodo-L-ascorbic acid for the in vivo study of ascorbate: autoradiography, biodistribution in normal and hypolipidemic rats, and in tumor-bearing nude mice
    Jintaek Kim
    Graduate School of Pharmaceutical Sciences, 3 1 1 Maidashi, Higashi ku, Fukuoka 812 8582, Japan
    Biol Pharm Bull 32:1906-11. 2009
    ....
  25. ncbi request reprint Ascorbate analogs for use in medical imaging: synthesis and radical scavenging activity of 5-O-(4'-iodobenzyl)-L-ascorbic acid
    Hiroharu Kato
    Graduate School of Pharmaceutical Sciences, Kyushu University, 3 1 1 Maidashi, Higashi ku, Fukuoka 812 8582, Japan
    Chem Pharm Bull (Tokyo) 55:1700-3. 2007
    ..The scavenging activity of the p-iodobenzylated analog against 2,2-diphenyl-1-picrylhyrazyl (DPPH) radical was almost the same as that of L-ascorbic acid itself...
  26. doi request reprint A radiogallium-DOTA-based bivalent peptidic ligand targeting a chemokine receptor, CXCR4, for tumor imaging
    Kohei Sano
    Department of Biomolecular Recognition Chemistry, Graduate School of Pharmaceutical Sciences, Kyushu University, 3 1 1 Maidashi, Higashi ku, Fukuoka 812 8582, Japan Department of Patho Functional Bioanalysis, Graduate School of Pharmaceutical Sciences, Kyoto University, 46 29 Yoshida Shimoadachimachi, Sakyo ku, Kyoto 606 8501, Japan
    Bioorg Med Chem Lett 24:1386-8. 2014
    ..The incorporation of two CXCR4 antagonists to Ga-DOTA could be effective in detecting CXCR4-expressing tumors. ..
  27. ncbi request reprint In vivo imaging of brain dopaminergic neurotransmission system in small animals with high-resolution single photon emission computed tomography
    Hideo Saji
    Graduate School of Pharmaceutical Sciences, Kyoto University, Yoshida, Sakyo ku, Kyoto 606 8501, Japan
    Anal Sci 19:67-71. 2003
    ....
  28. doi request reprint Difference in brain distributions of carbon 11-labeled 4-hydroxy-2(1H)-quinolones as PET radioligands for the glycine-binding site of the NMDA ion channel
    Takeshi Fuchigami
    Graduate School of Pharmaceutical Sciences, Kyushu University, Higashi ku, Fukuoka 812 8582, Japan
    Nucl Med Biol 35:203-12. 2008
    ....
  29. ncbi request reprint Effect of carboxylation of N-terminal phenylalanine of (111)in-DTPA (diethylenetriaminepentaacetic acid)-octreotide on accumulation of radioactivity in kidney
    Hiromichi Akizawa
    Faculty of Pharmaceutical Sciences, Okayama University, Tsushima Naka, Okayama 700 8530, Japan
    Biol Pharm Bull 27:271-2. 2004
    ..This effect can be attributed to the reduction of lipophilicity and also the repulsive force arisen from the negative charge of renal brush border membrane...
  30. ncbi request reprint Estimation of oxygen metabolism in a rat model of permanent ischemia using positron emission tomography with injectable15O-O2
    Takashi Temma
    Department of Patho Functional Bioanalysis, Graduate School of Pharmaceutical Sciences, Kyoto University, Kyoto, Japan
    J Cereb Blood Flow Metab 26:1577-83. 2006
    ..Injectable (15)O-O(2) could be used to reliably estimate oxygen metabolism in an infarction rat model with positron emission tomography...
  31. ncbi request reprint Availability of N-isopropyl-p-[125I]iodoamphetamine (IMP) as a practical cerebral blood flow (CBF) indicator in rats
    Takashi Temma
    Department of Patho Functional Bioanalysis, Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo ku, Kyoto 606 8501, Japan
    Nucl Med Biol 31:811-4. 2004
    ..The results indicate that DUR of [125I]IMP at 5 min after injection in rats is a useful and practical indicator of CBF since neither arterial blood sampling nor metabolite correction is necessary...
  32. ncbi request reprint 1-(3'-[125I]Iodophenyl)-3-methy-2-pyrazolin-5-one: preparation, solution stability, and biodistribution in normal mice
    Yuuhei Sano
    Graduate School of Pharmaceutical Sciences, Kyushu University, 3 1 1 Maidashi, Higashi ku, Fukuoka, Japan
    Chem Pharm Bull (Tokyo) 58:1020-5. 2010
    ..Intravenous injection of (125)I-2 with low specific radioactivity into normal mice showed signs of distribution profiles similar to reported results for (14)C-labeled edaravone in normal rats...
  33. ncbi request reprint Lectin-like oxidized LDL receptor-1 (LOX-1) expression is associated with atherosclerotic plaque instability--analysis in hypercholesterolemic rabbits
    Seigo Ishino
    Department of Patho Functional Bioanalysis, Graduate School of Pharmaceutical Sciences, Kyoto University, Japan
    Atherosclerosis 195:48-56. 2007
    ....
  34. ncbi request reprint A Tc-99m-labeled long chain fatty acid derivative for myocardial imaging
    Yasuhiro Magata
    Department of Patho Functional Bioanalysis, Graduate School of Pharmaceutical Sciences, Kyoto University, Kyoto, Japan
    Bioconjug Chem 15:389-93. 2004
    ..In conclusion, [(99m)Tc]MAMA-HDA is a promising compound as a long chain fatty acid analogue for estimating beta-oxidation of fatty acid in the heart...
  35. ncbi request reprint Methoxy- and fluorine-substituted analogs of O-1302: synthesis and in vitro binding affinity for the CB1 cannabinoid receptor
    Shintaro Tobiishi
    Graduate School of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan
    Chem Pharm Bull (Tokyo) 55:1213-7. 2007
    ..A morpholine ring substituted at the C(3) of the pyrazole ring resulted in a reduction of the CB1 affinity...
  36. doi request reprint Radiolabeled γ-polyglutamic acid complex as a nano-platform for sentinel lymph node imaging
    Kohei Sano
    Department of Biomolecular Recognition Chemistry, Graduate School of Pharmaceutical Sciences, Kyushu University, 3 1 1 Maidashi, Higashi ku, Fukuoka 812 8582, Japan
    J Control Release 194:310-5. 2014
    ..Thus, (111)In-DTPA-G4/PEI/γ-PGA can be useful as a nano-platform for molecular imaging including sentinel LN imaging. ..
  37. ncbi request reprint Decreased tissue accumulation of 6-deoxy-6-[18F]fluoro-L-ascorbic acid in glutathione-deficient rats induced by administration of diethyl maleate
    Fumihiko Yamamoto
    Faculty of Pharmaceutical Sciences, Kyushu University Fukuoka 812 8582, Japan
    Biol Pharm Bull 28:1943-7. 2005
    ..The possible biological mechanisms, including competition with endogenous AA and ascorbate recycling, that modulate the uptake and accumulation into tissues of 18F-DFA and 14C-AA in GSH-deficient rats are discussed...
  38. doi request reprint Synthesis and in vitro evaluation of radioiodinated indolequinones targeting NAD(P)H: quinone oxidoreductase 1 for internal radiation therapy
    Junichi Sasaki
    Graduate School of Pharmaceutical Sciences, Kyushu University, 3 1 1 Maidashi, Higashi ku, Fukuoka 812 8582, Japan
    Bioorg Med Chem 22:6039-46. 2014
    ..These data suggest that the novel NQO1-targeted radioiodinated compound [(125)I]3 could be used as a novel internal radiation agent for the treatment of cancer...
  39. ncbi request reprint Evaluation of radioiodinated 5-iodo-3-(2(S)-azetidinylmethoxy)pyridine as a ligand for SPECT investigations of brain nicotinic acetylcholine receptors
    Hideo Saji
    Graduate School of Pharmaceutical Sciences, Kyoto University, Japan
    Ann Nucl Med 16:189-200. 2002
    ..These results suggested that [123I]5IA is a promising radiopharmaceutical for SPECT studies of central nAChRs in human subjects...
  40. doi request reprint Interactions of a Tetrazine Derivative with Biomembrane Constituents: A Langmuir Monolayer Study
    Hiromichi Nakahara
    Department of Biophysical Chemistry, Graduate School of Pharmaceutical Sciences, Nagasaki International University, 2825 7 Huis Ten Bosch, Sasebo, Nagasaki 859 3298, Japan
    Langmuir 32:6591-9. 2016
    ..From these morphological observations, it is worthy to note that rTz-C18 is possible to interact with a limited amount of the lipids except for DPPE. ..
  41. ncbi request reprint Control of radioactivity pharmacokinetics of 99mTc-HYNIC-labeled polypeptides derivatized with ternary ligand complexes
    Masahiro Ono
    Department of Patho Functional Bioanalysis, Graduate School of Pharmaceutical Sciences, Kyoto University, Yoshida Shimoadachi cho, Sakyo Ku 606 8501, Japan
    Bioconjug Chem 13:491-501. 2002
    ..Thus, as ternary ligands facilitate alteration of the physicochemical properties of radiometabolites, the use of ternary ligand complexes might be applicable for controlling the pharmacokinetics of 99mTc-labeled polypeptides...
  42. ncbi request reprint Absorption characteristics of model compounds with different molecular weights from the serosal caecal surface in rats
    Koyo Nishida
    School of Pharmaceutical Sciences, Nagasaki University, Japan
    J Pharm Pharmacol 54:1005-9. 2002
    ..3, 0.5 and 1 mg), suggesting linear absorption. Moreover, the absorption ratios of FDs from the rat serosal caecal surface at 3 h decreased with an increase in the molecular weight (24.7% for FD4, 12.8% for FD-10 and 3.4% for FD-40)...
  43. ncbi request reprint A novel method for preparation of animal models of liver damage: liver targeting of carbon tetrachloride in rats
    Takahiro Mukai
    School of Pharmaceutical Sciences, Nagasaki University, Nagasaki, Japan
    Biol Pharm Bull 25:1494-7. 2002
    ....
  44. ncbi request reprint Quantitative fluorine 18 deoxyglucose uptake by myocardial positron emission tomography in rats
    Nobuhiro Handa
    Department of Thoracic and Cardiovascular Surgery, Kobe City General Hospital, Kobe, Japan
    J Nucl Cardiol 9:616-21. 2002
    ..Our objective was to assess whether FDG uptake measured by PET is correlated with tissue radioactivity of FDG in rat heart directly measured by an automated gamma counter...
  45. ncbi request reprint Kidney- and site-selective delivery of 5-fluorouracil utilizing the absorption on the kidney surface in rats
    Shigeru Kawakami
    School of Pharmaceutical Sciences, Nagasaki University, Japan
    Biol Pharm Bull 25:928-30. 2002
    ..The blood concentration of 5-FU was low (<1.7 microg/ml) until 120 min after kidney surface application. The maximum blood concentration of 5-FU after kidney surface application was much lower than after intravenous administration...
  46. ncbi request reprint Direct electrophilic radiofluorination of a cyclic RGD peptide for in vivo alpha(v)beta3 integrin related tumor imaging
    Mikako Ogawa
    Department of Biofunctional Research, National Institute for Longevity Sciences, Gengo, Morioka cho, Obu 474 8522, Japan
    Nucl Med Biol 30:1-9. 2003
    ..In tumor-bearing mice, the labeled peptides accumulated at the tumor with a high tumor to blood ratio. These findings suggest that an assessment of tumor characteristics may be obtained by using these (18)F-labeled peptides...
  47. pmc Differential uptake of (18)F-fluorodeoxyglucose by experimental tumors xenografted into immunocompetent and immunodeficient mice and the effect of immunomodification
    Marcelo Mamede
    Department of Nuclear Medicine and Diagnostic Imaging, Graduate School of Medicine, Kyoto University, 54 Kawahara cho, Shogoin, Sakyo ku, Kyoto, Japan
    Neoplasia 5:179-83. 2003
    ..To study the contribution of immunologic background to the uptake of fluorine-18-fluorodeoxyglucose ((18)F-FDG) by the tumor tissues...
  48. ncbi request reprint Clinical value of FDG-PET in the follow up of post-operative patients with endometrial cancer
    Tsuneo Saga
    Department of Nuclear Medicine and Diagnostic Imaging, Graduate School of Medicine, Kyoto University, Japan
    Ann Nucl Med 17:197-203. 2003
    ..The clinical usefulness of FDG-PET in the follow up of post-operative patients with endometrial cancer was retrospectively evaluated...
  49. ncbi request reprint Stomach- and site-selective delivery of 5-fluorouracil following its application on the gastric serosal surface in rats
    Junzo Nakamura
    Graduate School of Biomedical Sciences, Nagasaki University, Japan
    Biol Pharm Bull 28:1049-53. 2005
    ..Thus, the stomach- and site-selective delivery system following application on the gastric serosal surface could be applied with anticancer drugs for the treatment of gastric cancer...
  50. ncbi request reprint Quantification of human nicotinic acetylcholine receptors with 123I-5IA SPECT
    Marcelo Mamede
    Department of Nuclear Medicine and Diagnostic Imaging, Graduate School of Medicine, Kyoto University, Kyoto, Japan
    J Nucl Med 45:1458-70. 2004
    ..123I-5IA shows higher affinity toward the nAChR alpha4beta2 subtype, enhanced receptor subtype selectivity, good safety, and low nonspecific binding...
  51. ncbi request reprint Delivery advantage to the unilateral kidney by direct drug application to the kidney surface in rats and pharmacokinetic verification based on a physiological model
    Koyo Nishida
    Department of Clinical Pharmacy, Graduate School of Biomedical Sciences, Nagasaki University, 1 14 Bunkyo machi, Nagasaki, 852 8521, Japan
    J Drug Target 13:215-23. 2005
    ..Moreover, the delivery advantage of kidney surface application of PSP was verified by its comparison with other routes such as i.v. and i.a. administrations...
  52. ncbi request reprint Regional delivery of model compounds and 5-Fluorouracil to the liver by their application to the liver surface in rats: its implication for clinical use
    Koyo Nishida
    Department of Clinical Pharmacy, Graduate School of Biomedical Sciences, Nagasaki University, 1 14 Bunkyo machi, Nagasaki, 852 8521, Japan
    Pharm Res 22:1331-7. 2005
    ..The purpose of this study was to examine drug distribution in the liver after drug application to the rat liver surface...
  53. ncbi request reprint (18)F-FDG accumulation in atherosclerotic plaques: immunohistochemical and PET imaging study
    Mikako Ogawa
    Department of Investigative Radiology, Research Institute, National Cardiovascular Center, Suita, Japan
    J Nucl Med 45:1245-50. 2004
    ..Furthermore, PET imaging of vulnerable plaques was performed with an animal model of atherosclerosis, Watanabe heritable hyperlipidemic (WHHL) rabbits...
  54. ncbi request reprint What is the most appropriate scan timing for intraoperative detection of malignancy using 18F-FDG-sensitive gamma probe? Preliminary phantom and preoperative patient study
    Tatsuya Higashi
    Department of Nuclear Medicine and Diagnostic Imaging, Kyoto University Graduate School of Medicine, Japan
    Ann Nucl Med 18:105-14. 2004
    ..To evaluate the appropriate post-injection timing for hand-held-gamma-ray-detecting probe (GDP) scanning for the intraoperative detection of malignancy after preoperative F-18 FDG (FDG) injection...
  55. ncbi request reprint A catheter-based radiation detector for endovascular detection of atheromatous plaques
    Takahiro Mukai
    Department of Nuclear Medicine and Diagnostic Imaging, Graduate School of Medicine, Kyoto University, Kyoto, Japan
    Eur J Nucl Med Mol Imaging 31:1299-303. 2004
    ..In this study, we developed a charged particle-sensitive detector for the endovascular detection of small plaques...
  56. ncbi request reprint Evaluation of primary brain tumors with FLT-PET: usefulness and limitations
    Tsuneo Saga
    Department of Diagnostic Imaging and Nuclear Medicine, Graduate School of Medicine, Kyoto University, Kyoto, Japan
    Clin Nucl Med 31:774-80. 2006
    ..The purpose of this report was to investigate the potential of positron emission tomography using F-18 fluorodeoxythymidine (FLT-PET) in evaluating primary brain tumors...
  57. ncbi request reprint Absorption of phenolsulfonphthalein as a model across the mesenteric surface in rats to determine the drug absorption route after intraperitoneal administration
    Koyo Nishida
    Department of Clinical Pharmacy, Graduate School of Biomedical Sciences, Nagasaki University, 1 14 Bunkyo machi, Nagasaki 852 8521, Japan
    J Pharm Pharmacol 56:683-7. 2004
    ....
  58. ncbi request reprint Temporal change in human nicotinic acetylcholine receptor after smoking cessation: 5IA SPECT study
    Marcelo Mamede
    Department of Diagnostic Imaging and Nuclear Medicine, Graduate School of Medicine, Kyoto University, Kyoto, Japan
    J Nucl Med 48:1829-35. 2007
    ..However, changes in nAChRs after cigarette smoking cessation in humans are poorly understood. The aim of this study was to detect the dynamic changes of nAChRs after smoking and smoking cessation in the brains of living subjects...
  59. ncbi request reprint Quantitative FDG-uptake by positron emission tomography in progressive hypertrophy of rat hearts in vivo
    Nobuhiro Handa
    Department of Cardiovascular Surgery, Kyoto University Graduate School of Medicine, 54 Kawaharacho, Shogoin, Sakyo ku, Kyoto, 606 8507, Japan
    Ann Nucl Med 21:569-76. 2007
    ..Quantitative myocardial fluorodeoxyglucose positron emission tomography (FDG-PET) for assessing glucose uptake in vivo is reliable in normal rat heart...
  60. ncbi request reprint Further studies on the kidney- and site-selective delivery of 5-fluorouracil following kidney surface application in rats
    Junzo Nakamura
    Graduate School of Biomedical Sciences, Nagasaki University, Nagasaki, Japan
    Biol Pharm Bull 26:1761-4. 2003
    ..It was further elucidated that kidney surface application of this drug in rats results in its the kidney- and site-selective delivery...
  61. ncbi request reprint [Design of radiolabeled antibody fragments for tumor-selective radioactivity localization--brush border enzyme-sensitive bond to decrease renal accumulation of radioactivity]
    Takahiro Mukai
    Department of Nuclear Medicine and Diagnostic Imaging, Graduate School of Medicine, Kyoto University, 54 Shogoin, Kawahara cho, Sakyo ku, Kyoto 606 8507, Japan
    Yakugaku Zasshi 123:647-52. 2003
    ..These findings indicate that HML is a useful reagent for reducing the renal radioactivity levels of antibody fragments...
  62. ncbi request reprint 18F-FDG and 11C-methionine PET for evaluation of treatment response of lung cancer after stereotactic radiotherapy
    Takayoshi Ishimori
    Department of Nuclear Medicine and Diagnostic Imaging, Graduate School of Medicine, Kyoto University, Japan
    Ann Nucl Med 18:669-74. 2004
    ..Although the addition of Met-PET did not provide additional information over FDG-PET, FDG- and Met-PET could be used to evaluate the treatment effect of SRT...