Synthesis and biological evaluation of new 4-arylpiperidines and 4-aryl-4-piperidinols: dual Na+ and Ca 2+ channel blockers with reduced affinity for dopamine D 2 …

…, A Miyajima, Y Tamura-Horikawa, S Tamura

文献索引：Annoura, Hirokazu; Nakanishi, Kyoko; Uesugi, Mayumi; Fukunaga, Atsuko; Imajo, Seiichi; Miyajima, Atsuko; Tamura-Horikawa, Yoshiko; Tamura, Shigeki Bioorganic and Medicinal Chemistry, 2002 , vol. 10, # 2 p. 371 - 383

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被引用次数: 32

摘要

A series of novel 4-arylpiperidines and 4-aryl-4-piperidinols (2a–f, 3a–f and 4a–f) was synthesized and evaluated for blocking effects on both neuronal Na+ and T-type Ca2+ channels and binding affinity for dopamine D2 receptors. Most of the compounds blockaded both ion channels with potency greater than or equal to flunarizine 1a which was adopted as a reference standard. In addition, these compounds had significantly reduced affinity for ...