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Measurement of Brain Concentration of FK960 for Development of a Novel Antidementia Drug: A PET Study in Conscious Rhesus Monkeys

Akihiro Noda, MS1,2,3, Hiroyuki Takamatsu, PhD1,4, Yoshihiro Murakami, MS1,3, Kazuyoshi Yajima, PhD1,3, Mitsuyoshi Tatsumi1, Rikiya Ichise1 and Shintaro Nishimura, PhD1,3

1 The Medical and Pharmacological Research Center Foundation, Hakui, Japan
2 Department of Biotracer Medicine, Kanazawa University Graduate School of Medical Sciences, Kanazawa, Japan
3 Advanced Technology Platform Research Laboratory, Fujisawa Pharmaceutical Company, Ltd., Tsukuba, Japan
4 Medicinal Biology Research Laboratories, Fujisawa Pharmaceutical Company, Ltd., Osaka, Japan



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FIGURE 1. Chemical structure of FK960 (N-(4-acetyl-1-piperazinyl)-p-fluorobenzamide monohydrate). Asterisk denotes position of 18F labeling.

 


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FIGURE 2. Typical PET images obtained from 30 to 90 min after administration of 18F-FK960 preparation. Presented images are 3.6-mm transverse slices, and slice 6 corresponds to orbitomeatal plane.

 


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FIGURE 3. Time–concentration curves for plasma and brain after peroral administration of FK960 (0.1 mg/kg) containing 18F-FK960 (366 ± 14 MBq). Data are presented as mean + SE, averaged over all subjects (n = 3), at each point.

 





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