Abstract
The antagonist activities of some cyclohexylaralkylamines derived from perhexiline on the fast Na + channel and slow Ca 2+ channel in rat brain and rat heart were examined and compared to the antagonist activities of nifedipine, verapamil, prenylamine and perhexiline. Prenylamine, perhexiline and the cyclohexylaralkylamine derivatives inhibited the [ 3H]batrachotoxinin A 20-α-benzoate binding more than the [ 3H]nitrendipine binding in rat brain. The nature of the interaction of the cyclohexylaralkylamines with the binding of [ 3H]batrachotoxinin and [ 3H]nitreadipine was non-competitive. The synaptosomal 22Na uptake induced by protoveratrine B, a Na + channel agoaist, was also inhibited. Prenylamine, perhexiline and perhexiline derivatives were more potent on the fast Na + channel than on the Ca 2+ channel in contrast to nifedipine and verapamil. The inhibition of Na + and Ca 2+ channels was also shown in guinea pig left atria. Perhexiline, prenylamine and the perhexiline derivatives inhibited the protoveratrine B-induced contraction more than they inhibited that induced by CaCl 2, in contrast with nifedipine and verapamil. Our results showed that prenylamine, perhexiline and its related cyclohexylaralkylamines inhibited the fast Na + channel far more than the slow Ca 2+ channel in rat brain, rat heart and guinea pig atria.
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