| Abstract
| - Dequalinium is a potent and selective blocker of the smallconductance Ca2+-activated K+(SKCa)channel in rat sympathetic neurones. Analogues of dequaliniumpossessing 3−6, 8, 10, and12 methylene groups in the linking chain have been synthesized andtested for inhibition ofthe afterhyperpolarization in rat sympathetic neurones. Thecompounds having a 5−12-carbonchain showed very little variation in their activity asSKCa channel blockers. The analoguespossessing four and three methylenes exhibited 3- and 8-fold lowerpotency, respectively,compared with dequalinium. These results are discussed in thecontext of possible modes ofbinding of the compounds to the SKCa channel.
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