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

Research output: Contribution to journalArticlepeer-review

4 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)1570-1573
Number of pages4
JournalBiological and Pharmaceutical Bulletin
Volume26
Issue number11
DOIs
Publication statusPublished - Nov 2003

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Pharmaceutical Science

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