N-(phthalimidoalkyl) derivatives of serotonergic agents: a common interaction at 5-HT1A serotonin binding sites?

RA Glennon, NA Naiman, ME Pierson…

文献索引：Glennon, Richard A.; Naiman, Noreen A.; Pierson, M. Edward; Smith, J. Doyle; Ismaiel, Abd M.; et al. Journal of Medicinal Chemistry, 1989 , vol. 32, # 8 p. 1921 - 1926

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被引用次数: 54

摘要

We have previously examined a series of arylpiperazine derivatives 1 and have demonstrated that introduction of an N-(phthalimidobutyl)(NBP) group at the terminal amine not only is tolerated but can result in significantly enhanced (> lO-fold) affinities at 5-HT l~ sites relative to those derivatives where R= H. 6 Indeed, the arylpiperazine 6a (NAN-190) represents one of the highest affinity 5-HTlA agents (Ki= 0.6 nM) reported to Our working ...