16 research outputs found

    Synthesis and biological evaluation of radio-iodinated benzimidazoles as SPECT imaging agents for NR2B subtype of NMDA receptor.

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    In this study, the benzimidazole derivatives were synthesized and evaluated as imaging agents for the NR2B subtype of NMDA receptor. Among these ligands, 2-{[4-(4-iodobenzyl)piperidin-1-yl]methyl}benzimidazol-5-ol (8) and N-{2-[4-(4-iodobenzyl)-piperidin-1-ylmethyl]benzoimidazol-5-yl}-methanesulfonamide (9) exhibited high affinity for the NR2B subunit (K(i) values; 7.28 nM for 8 and 5.75 nM for 9). In vitro autoradiography experiments demonstrated high accumulation in the forebrain regions but low in the cerebellum for both [(125)I]8 and [(125)I]9. These regional distributions of the radioligands correlated with the expression of the NR2B subunit. The in vitro binding of these ligands was inhibited by NR2B antagonist but not by other site ligands, which suggested the high selectivity of [(125)I]8 and [(125)I]9 for the NR2B subunit. In mice, the regional brain uptakes of [(125)I]8 and [(125)I]9 at 5-180 min after administration were 0.42-0.56% and 0.44-0.67% dose/g, respectively. The brain-to-blood ratio of [(125)I]8 at 180 min was reduced by 34% in the presence of non-radioactive ligands and by 59% in the presence of the NR2B ligand Ro-25,6981. These results indicated that [(125)I]8 could be partially bound to the NR2B subunit in vivo. Although the brain uptake of these benzimidazole derivatives was too low to allow for in vivo SPECT imaging, these compounds might be useful scaffolds for the development of imaging probes specific for the NMDA receptors

    The Emergence of a Contemporary Repertoire for the Shō

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    The shō has played an important role in the creation of Japanese cultural identity. In examining this issue, we show the emancipation of contemporary shō repertoire in the last three decades. We outline the process of the creation of the cultural identity of shō from a historical perspective, explaining the physical structure, music tradition, and contemporary shō music. Shō has unique names for each bamboo pipe and each harmony. The limited number of shō harmonies determines traditional sound images. Some contemporary composers have collaborated to create original repertoires for shō; Maki Ishii, Toshi Ichiyanagi, Cort Lippe, Motoharu Kawashima.Le shō a joué un rôle important dans la création d’une identité culturelle japonaise. Nous argumentons l’émancipation du répertoire contemporain de shō au cours des trois dernières décennies. Nous précisons le processus de création de l’identité culturelle du shō à travers une perspective historique détaillant la structure physique du shō, sa tradition musicale, ainsi que sa musique contemporaine. Chaque bambou et chaque harmonie du shō possède un nom unique. Le nombre limité des harmonies de cet instrument caractérise les images sonores traditionnelles. Certains compositeurs contemporains ont collaboré à générer des répertoires originaux pour le shō : Maki Ishii, Toshi Ichiyanagi, Cort Lippe, Motoharu Kawashima

    ヘンデル《快活の人、沈思の人、中庸の人》の歌詞とその発音 : 第3部の場合

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    ヘンデルの《快活の人、沈思の人、中庸の人》は劇場音楽の形式に則り3部構成となっている。第1部と第2部の歌詞はミルトンの『快活の人』と『沈思の人』の詩句がそのまま用いられていて、第3部は台本作家ジェネンズが新たに書き下ろした歌詞が使われている。歌詞の割り振り方を見ると、第1部と第2部はそのミルトンの発音が採用されていてヘンデル時代から見ると古風な発音となっているが、第3部ではそれより新しい作曲当時の発音が使われていることが分かる。本稿では第3部について当時の発音を推定するとともにヘンデルの歌詞の表現について考察し歌詞の対訳を試みた
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