A novel class of Na+ and Ca2+ channel dual blockers with highly potent anti-ischemic effects |
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| Authors: | Annoura H Nakanishi K Uesugi M Fukunaga A Miyajima A Tamura-Horikawa Y Tamura S |
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| Affiliation: | Suntory Institute for Biomedical Research, Osaka, Japan. |
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| 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. |
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