Abstract:
:SK channels are small conductance, Ca(2+)-activated K(+) channels that underlie neuronal slow afterhyperpolarization and mediate spike frequency adaptation. Using the patch clamp technique, we tested the effects of eight clinically relevant psychoactive compounds structurally related to the tricyclic antidepressants, on SK2 subtype channels cloned from rat brain and functionally expressed in the human embryonic kidney cell line, HEK293. Amitriptyline, carbamazepine, chlorpromazine, cyproheptadine, imipramine, tacrine and trifluperazine blocked SK2 channel currents with micromolar affinity. The block was reversible and concentration-dependent. The potency differed according to chemical structure. In contrast, the cognitive enhancer linopirdine was ineffective at blocking these channels. Our results point to a distinct pharmacological profile for SK channels.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Dreixler JC,Bian J,Cao Y,Roberts MT,Roizen JD,Houamed KMdoi
10.1016/s0014-2999(00)00401-5keywords:
subject
Has Abstractpub_date
2000-07-28 00:00:00pages
1-7issue
1eissn
0014-2999issn
1879-0712pii
S0014299900004015journal_volume
401pub_type
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