PMID: 9660091Jul 11, 1998Paper

In vitro and in vivo characterization of (+)-3-[11C]cyano-dizocilpine

Journal of Neural Transmission
S SihverY Watanabe

Abstract

(+)-3-[11C]Cyano-5-methyl-10,11 -dihydro-5H-dibenzo[a,d]-cyclohepten-5,10-imine ([11C]MKC) was successfully synthesized as a potential radiotracer for PET studies on the NMDA receptor channel complex. In vitro binding properties of [11C]MKC were investigated with newly developed techniques for efficient evaluation of 11C-labeled compounds. The association curve of [11C]MKC binding in rat forebrain membranes showed that the specific binding reached an equilibrium within 30 min. Specific binding was saturable with affinity constant KD=8.2+/-0.4nM and Bmax=1.62+/-0.04 pmol/mg protein with glutamate and glycine included in the incubation medium. The binding of [11C]MKC was decreased by extensive washing of the membrane preparation. (+)- and (-)-Dizocilpine, 3-cyano-dizocilpine, and ketamine inhibited the specific binding of [11C]MKC with IC50 values of 37.3, 445.0, 65.8nM and 3.91 microM, respectively. High specific binding in in vitro autoradiography was distributed predominantly in telencephalic regions (the hippocampus, cerebral cortex, and striatum) followed by thalamus. PET studies using rhesus monkeys under anesthesia showed high uptake of [11C]MKC in the temporoparietal and frontal cerebral cortices, striatum, and thalamic r...Continue Reading

Citations

Dec 31, 2002·Journal of Receptor and Signal Transduction Research·Marko KokicSimon M Ametamey
Apr 16, 2015·TheScientificWorldJournal·Takeshi FuchigamiSakura Yoshida
May 29, 2000·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·Z PfundG J Moore
Sep 18, 2002·Drug and Alcohol Dependence·Michael A TaffeLisa H Gold

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