Synthesis, radiosynthesis and in vivo evaluation of 5-[3-(4-benzylpiperidin-1-yl) prop-1-ynyl]-1, 3-dihydrobenzoimidazol-2-[11 C] one, as a potent NR 1A/2B subtype …

…, Y Bramoullé, C Coulon, M Ottaviani, M Kassiou…

文献索引：Roger, Gaelle; Lagnel, Beatrice; Besret, Laurent; Bramoulle, Yann; Coulon, Christine; Ottaviani, Michelle; Kassiou, Michael; Bottlaender, Michel; Valette, Heric; Dolle, Frederic Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 24 p. 5401 - 5408

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被引用次数: 23

摘要

Recently, a new series of potent and highly subtype-selective 1-(heteroarylalkynyl)-4- benzylpiperidine antagonists of the NMDA receptors has been described by Pfizer Laboratories. In this series, 5-[3-(4-benzylpiperidin-1-yl) prop-1-ynyl]-1, 3- dihydrobenzoimidazol-2-one (1) was identified as a selective antagonist for the NR1A/2B subtype, displaying IC50 values for inhibition of the NMDA responses of 5.3 nM for this ...