Abstract:
AIM:To examine whether selective serotonin reuptake inhibitor citalopram interacts with Kv1.5, one of the cardiovascular-specific Kv channel isoforms. METHODS:The interaction between citalopram and Kv1.5 expressed in Chinese hamster ovary cells was studied using the whole-cell patch-clamp technique. RESULTS:Citalopram reduced Kv1.5 whole-cell currents in a reversible concentration-dependent manner, with an IC(50) value and a Hill coefficient of 2.8+/-1.1 micromol/L and 0.8+/-0.3, respectively. Citalopram-induced inhibition of Kv1.5 is associated with time-dependent development of block without modifying the kinetics of current activation. The inhibition increased steeply between -30 and 0 mV, which corresponded with the voltage range for channel opening. In the voltage range positive to 0 mV, inhibition displayed an additional voltage dependence, consistent with an electrical distance delta of 0.19. Citalopram slowed the deactivation time course, resulting in a tail crossover phenomenon when the tail currents, recorded in the presence and absence of citalopram, were superimposed. Inhibition of Kv1.5 by citalopram was use-dependent. CONCLUSION:The present results suggest that citalopram acts on Kv1.5 currents as an open-channel blocker, and much caution about arrhythmogenic risk is required when using citalopram in the treatment with depressed patients.
journal_name
Acta Pharmacol Sinjournal_title
Acta pharmacologica Sinicaauthors
Lee HM,Hahn SJ,Choi BHdoi
10.1038/aps.2010.14subject
Has Abstractpub_date
2010-04-01 00:00:00pages
429-35issue
4eissn
1671-4083issn
1745-7254pii
aps201014journal_volume
31pub_type
杂志文章abstract::Anlotinib is a new oral tyrosine kinase inhibitor; this study was designed to characterize its pharmacokinetics and disposition. Anlotinib was evaluated in rats, tumor-bearing mice, and dogs and also assessed in vitro to characterize its pharmacokinetics and disposition and drug interaction potential. Samples were ana...
journal_title:Acta pharmacologica Sinica
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abstract:AIM:To explore the action of doxorubicin on vascular smooth muscle cells. METHODS:Isometric tension of denuded or intact thoracic aortic vessels was recorded and [Ca(2+)](i) in isolated aortic smooth muscle cells was measured by using Fluo-3. RESULTS:Doxorubicin induced phasic and tonic contractions in denuded vessel...
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journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章,评审
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abstract:AIM:To investigate the metabolic characteristics of cytochrome P-450 C YP2A6 in human liver microsomes. METHODS:Cytochrome P-450 enzyme activities were measured by biochemical assays. Xenobiotics were employed to observe their effects on CYP2A6 in vitro. The kinetics of coumarin 7-hydroxylase was determined, and the c...
journal_title:Acta pharmacologica Sinica
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journal_title:Acta pharmacologica Sinica
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pub_type: 临床试验,杂志文章
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journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
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doi:
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pub_type: 杂志文章,评审
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doi:
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journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:10.1038/aps.2017.136
更新日期:2018-07-01 00:00:00
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doi:
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doi:10.1038/aps.2008.26
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pub_type: 杂志文章
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journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章,评审
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更新日期:2010-09-01 00:00:00
abstract:AIM:The feasibility of inducing endocrine pancreatic differentiation of embryonic stem (ES) cells has been well documented. However, whether ES cells possess the potential for exocrine pancreatic differentiation requires further exploration. Here, we investigated whether sodium butyrate and glucocorticoids were conduci...
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pub_type: 杂志文章
doi:10.1038/aps.2009.115
更新日期:2009-09-01 00:00:00
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journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
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journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:10.1038/aps.2012.100
更新日期:2012-10-01 00:00:00
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journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:10.1038/aps.2012.5
更新日期:2012-05-01 00:00:00
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journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章,评审
doi:10.1111/j.1745-7254.2006.00278.x
更新日期:2006-03-01 00:00:00
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journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:
更新日期:2003-04-01 00:00:00
abstract::Severe acute pancreatitis (SAP) is a severe acute abdominal disease. Recent evidence shows that intestinal homeostasis is essential for the management of acute pancreatitis. Chitosan oligosaccharides (COS) possess antioxidant activity that are effective in treating various inflammatory diseases. In this study we explo...
journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:10.1038/s41401-020-00581-5
更新日期:2021-01-25 00:00:00
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journal_title:Acta pharmacologica Sinica
pub_type: 杂志文章
doi:10.1111/j.1745-7254.2008.00745.x
更新日期:2008-05-01 00:00:00