88537-45-5Relevant articles and documents
Synthesis of 11C-labelled bis(phenylalkyl)amines and their in vitro and in vivo binding properties in rodent and monkey brains
Sasaki, Shigeki,Kurosaki, Fumie,Haradahira, Terushi,Yamamoto, Fumihiko,Maeda, Jun,Okauchi, Takashi,Suzuki, Kazutoshi,Suhara, Tetsuya,Maeda, Minoru
, p. 531 - 537 (2004)
Two new 11C-labelled ligands, N-(3-(4-hydroxyphenyl)propyl)-3- (4-methoxyphenyl)propylamine ([11C]2) and N-(3-(4-hydroxyphenyl) butyl)-3-(4-methoxyphenyl)butylamine ([11C]3) were designed based on bis(phenylalkyl)-amines (1) which have been reported as polyamine site antagonists with high-selectivity for NR1A/2B NMDA receptors, and radiolabelling of the corresponding phenol precursors with [11C]methyl iodide was readily accomplished. The in vitro inhibition experiments using rat brain slices showed that [11C]2 and [11C]3 share the binding sites with spermine and/or ifenprodil but not with CP-101,606, a highly potent NR2B-selective NMDA antagonist, and that divalent cations such as Zn 2+ produced significant inhibition of both [11C]2 and [11C]3 bindings. Intravenous injection of [11C]3 in mice showed almost homogenous distribution throughout the brain. Attempts to block the tracer uptake of [11C]3 by pre-injection with the unlabelled 3 or spermine in rats were unsuccessful, but a small decrease in the cerebral uptake of [11C]3 by co-treatment with the unlabelled 3 was observed in a monkey PET study. The present findings indicate that none of these 11C-labelled analogues have potential for PET study of binding sites on the N-methly-D-aspartate (NMDA) receptors.
SODIUM CHANNEL BLOCKERS
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, (2016/01/21)
The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.
Sodium channel blockers
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, (2008/06/13)
The present invention relates to sodium channel blockers. The present invention also relates to a variety of methods of treatment using the sodium channel blockers.