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 | |
| Publication status | Published - Nov 1 2003 |
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All Science Journal Classification (ASJC) codes
- Pharmacology
- Pharmaceutical Science
Cite this
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, 01.11.2003, p. 1570-1573.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Synthesis and brain regional distribution of [11C]NPS 1506 in mice and rat
T2 - An N-methyl-D-aspartate (NMDA) receptor antagonist
AU - Fuchigami, Takeshi
AU - Haradahira, Terushi
AU - Arai, Takuya
AU - Okauchi, Takashi
AU - Maeda, Jun
AU - Suzuki, Kazutoshi
AU - Yamamoto, Fumihiko
AU - Suhara, Tetsuya
AU - Sasaki, Shigeki
AU - Maeda, Minoru
PY - 2003/11/1
Y1 - 2003/11/1
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=19944431375&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=19944431375&partnerID=8YFLogxK
U2 - 10.1248/bpb.26.1570
DO - 10.1248/bpb.26.1570
M3 - Article
C2 - 14600403
AN - SCOPUS:19944431375
VL - 26
SP - 1570
EP - 1573
JO - Biological and Pharmaceutical Bulletin
JF - Biological and Pharmaceutical Bulletin
SN - 0918-6158
IS - 11
ER -