Synthesis and brain regional distribution of [11C]NPS 1506 in mice and rat: An N-methyl-D-aspartate (NMDA) receptor antagonist

Takeshi Fuchigami, Terushi Haradahira, Takuya Arai, Takashi Okauchi, Jun Maeda, Kazutoshi Suzuki, Fumihiko Yamamoto, Tetsuya Suhara, Shigeki Sasaki, Minoru Maeda

研究成果: Contribution to journalArticle査読

4 被引用数 (Scopus)

抄録

NPS 1506 [3-fluoro-γ-(3-fluorophenyl)-N-methylbenzenepropamine] is representative of a non-psychotomimetic class of N-methyl-D-aspartate (NMDA) receptor antagonists. [11C]NPS 1506 was prepared at high radiochemical purity (γ98%) with a specific activity of around 50 GBq/μmmol at the end of synthesis by methylation of the desmethyl precursor with [11C]methyl iodide in the presence of NaH. Biodistribution of [11C]NPS 1506 in mice and rat demonstrated that uptake into the brain was rapid and occurred at high levels. [11C]NPS 1506 showed no appreciable specific binding in rodent brains under in vivo conditions, possibly because of both a large non-specific bound fraction and low in vitro binding affinity for NMDA receptors.

本文言語英語
ページ(範囲)1570-1573
ページ数4
ジャーナルBiological and Pharmaceutical Bulletin
26
11
DOI
出版ステータス出版済み - 11 2003

All Science Journal Classification (ASJC) codes

  • 薬理学
  • 薬科学

フィンガープリント

「Synthesis and brain regional distribution of [<sup>11</sup>C]NPS 1506 in mice and rat: An N-methyl-D-aspartate (NMDA) receptor antagonist」の研究トピックを掘り下げます。これらがまとまってユニークなフィンガープリントを構成します。

引用スタイル