Abstract：
:1. The pharmacology of the slow afterhyperpolarization (sAHP) was studied in cultured rat hippocampal pyramidal neurones. 2. Clotrimazole, its in vivo metabolite, 2-chlorophenyl-bisphenyl-methanol (CBM) and the novel analogues, UCL 1880 and UCL 2027, inhibited the sI(AHP) with similar IC50s (1-2 microM). 3. Clotrimazole and CBM also inhibited the high voltage-activated (HVA) Ca2+ current in pyramidal neurones with IC50s of 4.7 microM and 2.2 microM respectively. UCL 1880 was a less effective Ca2+ channel blocker, reducing the HVA Ca2+ current by 50% at 10 microM. At concentrations up to 10 microM, UCL 2027 had no effect on the Ca2+ current, indicating that its effects on the sI(AHP) were independent of Ca2+ channel block. 4. Clotrimazole also inhibited both the outward holding current (IC50=2.8 microM) present at a potential of -50 mV and the apamin-sensitive medium AHP (mAHP; IC50 approximately amp;10 microM). The other clotrimazole analogues tested had smaller effects on these two currents. The present work also shows that 100 nM UCL 1848, an inhibitor of apamin-sensitive conductances, abolishes the mAHP. 5. Currents were recorded from HEK293 cells transfected with hSK1 and rSK2. The SK currents were very sensitive to inhibition by UCL 1848 but were not significantly reduced by the sI(AHP) inhibitor, UCL 2027 (10 microM). 10 microM UCL 1880 reduced the hSK1 current by 40%. 6. UCL 2027 appears to be the first relatively selective blocker of the sAHP to be described. Furthermore, the ability of UCL 2027 to block the sAHP with minimal effect on SK1 channel activity questions the role of this channel in the sAHP.
journal_name
Br J Pharmacoljournal_title
British journal of pharmacologyauthors
Shah MM,Miscony Z,Javadzadeh-Tabatabaie M,Ganellin CR,Haylett DGdoi
10.1038/sj.bjp.0703895subject
Has Abstractpub_date
2001-02-01 00:00:00pages
889-98issue
4eissn
0007-1188issn
1476-5381journal_volume
132pub_type
杂志文章abstract：:1. Strength-duration curves for threshold mechanical responses to single transmural stimuli were identical for rat and guinea-pig detrusor. In both species atropine had no effect on the curves, but the curves were shifted to the right by nerve blockade with tetrodotoxin (TTX), and by blockade of P2-purinoceptors with ...
journal_title：British journal of pharmacology
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doi：10.1111/j.1476-5381.1990.tb12956.x
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journal_title：British journal of pharmacology
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doi：10.1111/j.1476-5381.1996.tb15772.x
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journal_title：British journal of pharmacology
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doi：10.1111/j.1476-5381.2010.00792.x
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doi：10.1038/sj.bjp.0704691
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doi：10.1111/bph.14797
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doi：10.1038/sj.bjp.0705538
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journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.1982.tb08781.x
更新日期：1982-02-01 00:00:00
abstract：BACKGROUND AND PURPOSE:Two of the most relevant unmet needs in epilepsy are represented by the development of disease-modifying drugs able to affect epileptogenesis and/or the study of related neuropsychiatric comorbidities. No systematic study has investigated the effects of chronic treatment with antipsychotics or an...
journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/bph.13121
更新日期：2015-06-01 00:00:00
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journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.1994.tb13197.x
更新日期：1994-08-01 00:00:00
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pub_type： 杂志文章
doi：10.1111/j.1476-5381.1991.tb12290.x
更新日期：1991-04-01 00:00:00
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journal_title：British journal of pharmacology
pub_type： 临床试验,杂志文章
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更新日期：2001-11-01 00:00:00
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journal_title：British journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1111/bph.14464
更新日期：2019-02-01 00:00:00
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journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.1978.tb07794.x
更新日期：1978-07-01 00:00:00
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pub_type： 杂志文章
doi：10.1111/j.1476-5381.1992.tb14341.x
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journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.1987.tb11359.x
更新日期：1987-11-01 00:00:00
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journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.1987.tb08958.x
更新日期：1987-02-01 00:00:00
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journal_title：British journal of pharmacology
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doi：10.1038/sj.bjp.0706193
更新日期：2005-06-01 00:00:00
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更新日期：2002-02-01 00:00:00
abstract：:Prostanoids, generated from cyclooxygenase (COX) isoenzymes, play a role in the physiological function of the lower urinary tract and are important mediators of inflammatory hyperalgesia. The present work evaluates the effects of the COX-1/COX-2 inhibitor dexketoprofen as well as of a selective COX-2 inhibitor, NS-398...
journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1038/sj.bjp.0703309
更新日期：2000-05-01 00:00:00
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journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.1991.tb12386.x
更新日期：1991-09-01 00:00:00
abstract：:1. The aim of this study was to determine the response of porcine small pulmonary arteries to intralumenal flow and to identify the cellular mechanisms and potential mediators involved in the response. 2. Porcine small pulmonary arteries were isolated from a branch of the main intrapulmonary artery of the lower lung l...
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doi：10.1038/sj.bjp.0701846
更新日期：1998-05-01 00:00:00
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journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.1994.tb14796.x
更新日期：1994-03-01 00:00:00
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journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1038/sj.bjp.0702244
更新日期：1998-12-01 00:00:00
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journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.1992.tb09011.x
更新日期：1992-03-01 00:00:00
abstract：:1. The actions of etorphine, morphine and diprenorphine were investigated on neurones of the cerebral cortex and spinal cord of rats anaesthetized with pentobarbitone.2. In the cerebral cortex, intravenous etorphine increased the latency of the primary evoked response to a peripheral nerve stimulus and suppressed the ...
journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.1972.tb06865.x
更新日期：1972-10-01 00:00:00
abstract：:1. The effects of long-term treatment with trandolapril, an angiotensin I-converting enzyme inhibitor, on exercise capacity of rats with chronic heart failure (CHF) following coronary artery ligation were examined. CHF was developed by 8 weeks after the coronary artery ligation. 2. The running time of rats with CHF in...
journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1038/sj.bjp.0702471
更新日期：1999-04-01 00:00:00
