Subtype-selective N-methyl-D-aspartate receptor antagonists: synthesis and biological evaluation of 1-(heteroarylalkynyl)-4-benzylpiperidines

…, SA Espitia, CS Konkoy, ER Whittemore…

文献索引：Wright; Gregory; Kesten; Boxer; Serpa; Meltzer; Wise; Espitia; Konkoy; Whittemore; Woodward Journal of Medicinal Chemistry, 2000 , vol. 43, # 18 p. 3408 - 3419

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被引用次数: 78

摘要

4-[4-(4-Benzylpiperidin-1-yl) but-1-ynyl] phenol (8) and 4-[3-(4-benzylpiperidin-1-yl) prop-1- ynyl] phenol (9) are potent NR1a/2B receptor antagonists (IC50 values 0.17 and 0.10 μM, respectively). Administered intraperitoneally, they both potentiated the activity of l-DOPA in the unilaterally 6-hydroxydopamine-lesioned (6-OHDA) rat, a model of Parkinson's disease. However, compound 9 was not active orally, likely due to rapid first-pass metabolism of ...