PubMed 10915830
Referenced in: none
Automatically associated channels: SK2 , Slo1
Title: Block of rat brain recombinant SK channels by tricyclic antidepressants and related compounds.
Authors: J C Dreixler, J Bian, Y Cao, M T Roberts, J D Roizen, K M Houamed
Journal, date & volume: Eur. J. Pharmacol., 2000 Jul 28 , 401, 1-7
PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/10915830
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.