Research Topics flumazenil gaba modulators

Tiwari A, Fujinaga M, Yui J, Yamasaki T, Xie L, Kumata K, et al. Synthesis and evaluation of new (18)F-labelled acetamidobenzoxazolone-based radioligands for imaging of the translocator protein (18 kDa, TSPO) in the brain. Org Biomol Chem. 2014;12:9621-30 pubmed publisher Kumata K, Yui J, Xie L, Zhang Y, Nengaki N, Fujinaga M, et al. Radiosynthesis and preliminary PET evaluation of glycogen synthase kinase 3β (GSK-3β) inhibitors containing [(11)C]methylsulfanyl, [(11)C]methylsulfinyl or [(11)C]methylsulfonyl groups. Bioorg Med Chem Lett. 2015;25:3230-3 pubmed publisher..PET with [(11)C]1 and [(11)C]3 showed 2 fold higher brain uptake of radioactivity in a mouse model of cold water stress in which GSK-3β expression was increased, than in the controls. .. Fujinaga M, Yamasaki T, Nengaki N, Ogawa M, Kumata K, Shimoda Y, et al. Radiosynthesis and evaluation of 5-methyl-N-(4-[(11)C]methylpyrimidin-2-yl)-4-(1H-pyrazol-4-yl)thiazol-2-amine ([(11)C]ADX88178) as a novel radioligand for imaging of metabotropic glutamate receptor subtype 4 (mGluR4). Bioorg Med Chem Lett. 2016;26:370-374 pubmed publisher Zhang M, Maeda J, Furutsuka K, Yoshida Y, Ogawa M, Suhara T, et al. [18F]FMDAA1106 and [18F]FEDAA1106: two positron-emitter labeled ligands for peripheral benzodiazepine receptor (PBR). Bioorg Med Chem Lett. 2003;13:201-4 pubmed ..Ex vivo autoradiograms of [(18)F]FMDAA1106 and [(18)F]FEDAA1106 binding sites in the rat brains revealed that a high radioactivity was present in the olfactory bulb, the highest PBR density region in the brain. .. Shimoda Y, Fujinaga M, Hatori A, Yui J, Zhang Y, Nengaki N, et al. N-(3,4-Dimethylisoxazol-5-yl)piperazine-4-[4-(2-fluoro-4-[(11)C]methylphenyl)thiazol-2-yl]-1-carboxamide: A promising positron emission tomography ligand for fatty acid amide hydrolase. Bioorg Med Chem. 2016;24:627-34 pubmed publisher ..Higher than 90% of the total radioactivity in the rat brain was irreversible at 30min after the radioligand injection. The present results indicate that [(11)C]1 is a promising PET ligand for imaging of FAAH in living brain. .. Shimoda Y, Yui J, Fujinaga M, Xie L, Kumata K, Ogawa M, et al. [(11)C-carbonyl]CEP-32496: radiosynthesis, biodistribution and PET study of brain uptake in P-gp/BCRP knockout mice. Bioorg Med Chem Lett. 2014;24:3574-7 pubmed publisher ..Small-animal PET studies with [(11)C]CEP-32496 indicated that radioactivity levels (AUC0-90 min, SUV×min) accumulated in the brains of P-gp/BCRP knockout mice at a 8-fold higher rate than in the brains of wild-type mice...