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Synthesis of Fluorine-Containing Phosphodiesterase 10A (PDE10A) Inhibitors and the In Vivo Evaluation of F-18 Labeled PDE10A PET Tracers in Rodent and Nonhuman Primate

[Image: see text] A series of fluorine-containing PDE10A inhibitors were designed and synthesized to improve the metabolic stability of [(11)C]MP-10. Twenty of the 22 new analogues had high potency and selectivity for PDE10A: 18a–j, 19d–j, 20a–b, and 21b had IC(50) values <5 nM for PDE10A. Seven...

詳細記述

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書誌詳細
出版年:J Med Chem
主要な著者: Li, Junfeng, Zhang, Xiang, Jin, Hongjun, Fan, Jinda, Flores, Hubert, Perlmutter, Joel S., Tu, Zhude
フォーマット: Artigo
言語:Inglês
出版事項: 2015
主題:
オンライン・アクセス:https://ncbi.nlm.nih.gov/pmc/articles/PMC4697445/
https://ncbi.nlm.nih.gov/pubmed/26430878
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.5b01205
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