A novel class of Na+ and Ca 2+ channel dual blockers with highly potent anti-ischemic effects

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

Index: Annoura, Hirokazu; Nakanishi, Kyoko; Uesugi, Mayumi; Miyajima, Atsuko Fukunaga Atsuko; Tamura-Horikawa, Yoshiko; Tamura, Shigeki Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 20 p. 2999 - 3002

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Citation Number: 21

Abstract

A series of novel arylpiperidines (4a-d) which have highly potent blocking effects for both neuronal Na+ and T-type Ca2+ channels with extremely low affinity for dopamine D2 receptors were synthesized. Among these compounds, 1-(2-hydroxy-3-phenoxy) propyl-4-(4- phenoxyphenyl)-piperidine hydrochloride (4c; SUN N5030) exhibited remarkable neuroprotective activity in a transient middle cerebral artery occlusion (MCAO) model.