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 |
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Pages (from-to) | 1570-1573 |
Number of pages | 4 |
Journal | Biological and Pharmaceutical Bulletin |
Volume | 26 |
Issue number | 11 |
DOIs | |
Publication status | Published - Nov 2003 |
All Science Journal Classification (ASJC) codes
- Pharmacology
- Pharmaceutical Science