Crobenetine (BIII-890), a benzomorphan derivative, is a potent, selective, and highly use-dependent Na + channel blocker. Crobenetine displaces [3H] BTX from site 2 of the Na + channel (IC 50 =49 nM) in rat brain synaptosomes, yet exhibits only low binding affinity for other receptors and ion channels. Crobenetine protects brain tissue from the deleterious effects of focal cerebral ischemia in rodents.
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