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ID: ALA1131853

Journal: Bioorg Med Chem Lett

Title: A novel class of Na+ and Ca2+ channel dual blockers with highly potent anti-ischemic effects.

Authors: Annoura H, Nakanishi K, Uesugi M, Fukunaga A, Miyajima A, Tamura-Horikawa Y, Tamura S.

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.

CiteXplore: 10571163

DOI: 10.1016/s0960-894x(99)00516-8