Synthesis and brain regional distribution of [11C]NPS 1506 in mice and rat: an N-methyl-D-aspartate (NMDA) receptor antagonist.
NPS 1506 [3-fluoro-gamma-(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 (>98%) with a specific activity of around 50 GBq/micromol 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.
Graduate School of Pharmaceutical Sciences, Kyushu University, Maidashi, Fukuoka 812-8582, Japan.
Takeshi
T
Fuchigami
Terushi
T
Haradahira
Takuya
T
Arai
Takashi
T
Okauchi
Jun
J
Maeda
Kazutoshi
K
Suzuki
Fumihiko
F
Yamamoto
Tetsuya
T
Suhara
Shigeki
S
Sasaki
Minoru
M
Maeda
D000818:Animals; D001921:Brain / Q000378:metabolism*; D002250:Carbon Radioisotopes / Q000378:metabolism; D018691:Excitatory Amino Acid Antagonists / Q000138:chemical synthesis / Q000378:metabolism; D005464:Fluorobenzenes / Q000138:chemical synthesis* / Q000378:metabolism*; D008297:Male; D051379:Mice; D051381:Rats; D017207:Rats, Sprague-Dawley; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors* / Q000378:metabolism*
D002250:Carbon Radioisotopes; D018691:Excitatory Amino Acid Antagonists; D005464:Fluorobenzenes; D016194:Receptors, N-Methyl-D-Aspartate; C405105:NPS 1506