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

doi:10.1248/bpb.26.1570

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

Chemo-Pharmaceutical Sciences

Research output: Contribution to journal › Article › peer-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 language	English
Pages (from-to)	1570-1573
Number of pages	4
Journal	Biological and Pharmaceutical Bulletin
Volume	26
Issue number	11
DOIs	https://doi.org/10.1248/bpb.26.1570
Publication status	Published - Nov 2003

All Science Journal Classification (ASJC) codes

Pharmacology
Pharmaceutical Science

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Synthesis and brain regional distribution of [¹¹C]NPS 1506 in mice and rat : An N-methyl-D-aspartate (NMDA) receptor antagonist. / Fuchigami, Takeshi; Haradahira, Terushi; Arai, Takuya; Okauchi, Takashi; Maeda, Jun; Suzuki, Kazutoshi; Yamamoto, Fumihiko; Suhara, Tetsuya; Sasaki, Shigeki; Maeda, Minoru.

In: Biological and Pharmaceutical Bulletin, Vol. 26, No. 11, 11.2003, p. 1570-1573.

Research output: Contribution to journal › Article › peer-review

Fuchigami, Takeshi ; Haradahira, Terushi ; Arai, Takuya ; Okauchi, Takashi ; Maeda, Jun ; Suzuki, Kazutoshi ; Yamamoto, Fumihiko ; Suhara, Tetsuya ; Sasaki, Shigeki ; Maeda, Minoru. / Synthesis and brain regional distribution of [¹¹C]NPS 1506 in mice and rat : An N-methyl-D-aspartate (NMDA) receptor antagonist. In: Biological and Pharmaceutical Bulletin. 2003 ; Vol. 26, No. 11. pp. 1570-1573.

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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.",

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

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AU - Arai, Takuya

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AU - Maeda, Jun

AU - Suzuki, Kazutoshi

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