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.
MeSH terms
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Animals
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Anticonvulsants / pharmacology
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Calcium Channel Blockers / pharmacology*
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Calcium Channels, T-Type / drug effects*
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Epilepsy, Reflex / prevention & control
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Ischemic Attack, Transient / prevention & control*
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Mice
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Mice, Inbred DBA
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Neuroprotective Agents / pharmacology*
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Phenyl Ethers / pharmacology*
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Piperidines / pharmacology*
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Sodium Channel Blockers*
Substances
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Anticonvulsants
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Calcium Channel Blockers
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Calcium Channels, T-Type
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Neuroprotective Agents
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Phenyl Ethers
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Piperidines
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SUN N5030
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Sodium Channel Blockers