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

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.

• Authors: H Annoura, K Nakanishi, M Uesugi, A Fukunaga, A Miyajima, Y Tamura-Horikawa, S Tamura
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 9 Issue 20 Pg. 2999-3002 (Oct 18 1999) ISSN: 0960-894X [Print] England
• PMID: 10571163 (Publication Type: Journal Article)

Chemical References

• Anticonvulsants
• Calcium Channel Blockers
• Calcium Channels, T-Type
• Neuroprotective Agents
• Phenyl Ethers
• Piperidines
• SUN N5030
• Sodium Channel Blockers

Topics

• Animals
• Anticonvulsants (pharmacology)
• Calcium Channel Blockers (pharmacology)
• Calcium Channels, T-Type (drug effects)
• Epilepsy, Reflex (prevention & control)
• Ischemic Attack, Transient (prevention & control)
• Mice
• Mice, Inbred DBA
• Neuroprotective Agents (pharmacology)
• Phenyl Ethers (pharmacology)
• Piperidines (pharmacology)
• Sodium Channel Blockers