4-(Phosphonoalkyl)-and 4-(phosphonoalkenyl)-2-piperidinecarboxylic acids: synthesis, activity at N-methyl-D-aspartic acid receptors and anticonvulsant activity

…, R De Jesus, L Blanchard, RH Jackson…

文献索引：Hutchison; Williams; Angst; De Jesus; Blanchard; Jackson; Wilusz; Murphy; Bernard; Schneider; Campbell; Guida; Sills Journal of Medicinal Chemistry, 1989 , vol. 32, # 9 p. 2171 - 2178

全文：HTML全文

被引用次数: 88

摘要

A series of 4-(phosphonoalkyl)-and 4-(phosphonoalkenyl)-2-piperidinecarboxylic acids were synthesized, and their biological activity was assessed as competitive ligands for the NMDA receptor, both in vitro by using a receptor binding assay ([3H] CGS 19755 binding) and in vivo by using an NMDA seizure model in mice. The analogues were also evaluated in [3H] AMPA and [3H] kainate binding to assess their affinity for non-NMDA excitatory amino ...