Block of volume-regulated anion channels by selective serotonin reuptake inhibitors.

作者: Maertens C. , Droogmans G. , Verbesselt R. , Nilius B.

DOI: 10.1007/S00210-002-0567-5

关键词: Patch clampParoxetineChloride channelSertralineCitalopramPharmacologyChemistryMembrane potentialFluvoxamineSerotonin Uptake Inhibitors

摘要: We have used the whole-cell patch clamp technique to study effects of commonly antidepressants sertraline, paroxetine, citalopram and fluvoxamine on volume-regulated anion channel (VRAC) in endothelial cells. It was purpose present experiments investigate whether VRAC block is a general property this group selective serotonin reuptake inhibitors (SSRIs). At pH 7.4, all SSRIs induced fast reversible volume-sensitive chloride current (I Cl,swell), with an IC50 value 2.1±0.5 µM for 2.7±0.2 µM 12.3±1.4 µM 27.7±2.8 µM citalopram. The enhanced at more alkaline pH, indicating that it mediated by uncharged form. This describes variety channel. Our data reveal potent suggest hydrophobic interaction high affinity between SSRI channels. conclude pharmacological class inhibitors.

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