Identification of novel ligands for the gabapentin binding site on the α2δ subunit of a calcium channel and their evaluation as anticonvulsant agents

…, RJ Oles, JC O'Toole, GM Perkins…

文献索引：Bryans, Justin S.; Davies, Natasha; Gee, Nicolas S.; Dissanayake, Visaka U. K.; Ratcliffe, Giles S.; Horwell, David C.; Kneen, Clare O.; Morrell, Andrew I.; Oles, Ryszard J.; O'Toole, John C.; Perkins, Gemma M.; Singh, Lakhbir; Suman-Chauhan, Nirmala; O'Neill, Jacqueline A. Journal of Medicinal Chemistry, 1998 , vol. 41, # 11 p. 1838 - 1845

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被引用次数: 84

摘要

As part of a program to investigate the structure-activity relationships of Gabapentin (Neurontin), a number of alkylated analogues were synthesized and evaluated in vitro for binding to the Gabapentin binding site located on the α2δ subunit of a calcium channel. A number of other bridged and heterocyclic analogues are also reported along with their in vitro data. Two compounds showing higher affinity than Gabapentin were selected for ...