Abstract：
:The effects of 5-hydroxypropafenone (5-OH-P), the main metabolite of propafenone, were studied in guinea pig papillary muscles obtained from untreated animals and from animals pretreated with 5-OH-P, 3 mg/kg for 24 days. In untreated muscles perfused with 2.7 and 5.4 mM K+, 5-OH-P depressed action potential amplitude and Vmax, reduced the resting membrane potential, and prolonged the effective refractory period (ERP), but had no effect on the duration of the action potential (APD), recovery time (RT), or ERP/RT ratio. 5-OH-P also shifted the membrane responsiveness curve downward and to the left (i.e., in hyperpolarizing direction), prolonged the ERP/APD ratio, depressed the amplitude and Vmax, and shortened the duration of the slow action potentials induced by isoproterenol in K+-depolarized muscles. Pretreatment with 5-OH-P had no effect on phase 0 characteristics or resting membrane potential, but it shortened the APD, ERP, and RT and decreased the ERP/APD ratio. Further addition of 5-OH-P produced similar but more marked changes than in untreated muscles. In papillary muscles perfused with 10 mM K+, the depressant effects of 5-OH-P on phase 0 characteristics and ERP/APD ratio were potentiated. A slight lengthening of the APD was also observed. Because all these effects are similar to those previously described with propafenone, it is concluded that 5-OH-P is an active metabolite which exhibits class 1 antiarrhythmic effects and which may be responsible for some of the cardiodepressant and antiarrhythmic effects previously described for propafenone.
journal_name
J Cardiovasc Pharmacoljournal_title
Journal of cardiovascular pharmacologyauthors
Valenzuela C,Delgado C,Tamargo Jdoi
10.1097/00005344-198711000-00005subject
Has Abstractpub_date
1987-11-01 00:00:00pages
523-9issue
5eissn
0160-2446issn
1533-4023journal_volume
10pub_type
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journal_title：Journal of cardiovascular pharmacology
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journal_title：Journal of cardiovascular pharmacology
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abstract：:Ambulatory blood pressure monitoring (ABPM) is a particularly useful method for evaluating the effects of antihypertensive drugs. ABPM allows the therapeutic effect of an agent to be assessed continually by a large number of measurements, and the greater number of readings contributes to the higher degree of reproduci...
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journal_title：Journal of cardiovascular pharmacology
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doi：
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journal_title：Journal of cardiovascular pharmacology
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journal_title：Journal of cardiovascular pharmacology
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journal_title：Journal of cardiovascular pharmacology
pub_type： 杂志文章
doi：10.1097/00005344-198505000-00023
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journal_title：Journal of cardiovascular pharmacology
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journal_title：Journal of cardiovascular pharmacology
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journal_title：Journal of cardiovascular pharmacology
pub_type： 杂志文章
doi：10.1097/00005344-199907000-00002
更新日期：1999-07-01 00:00:00
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journal_title：Journal of cardiovascular pharmacology
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journal_title：Journal of cardiovascular pharmacology
pub_type： 杂志文章
doi：10.1097/00005344-199512000-00002
更新日期：1995-12-01 00:00:00
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journal_title：Journal of cardiovascular pharmacology
pub_type： 杂志文章
doi：
更新日期：1991-01-01 00:00:00
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journal_title：Journal of cardiovascular pharmacology
pub_type： 杂志文章
doi：
更新日期：1994-03-01 00:00:00
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journal_title：Journal of cardiovascular pharmacology
pub_type： 杂志文章
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更新日期：2015-04-01 00:00:00
abstract：:Acute exposure of human saphenous vein or internal thoracic artery endothelium to either morphine [27.4 +/- 3.7 and 35.4 +/- 4.1 nM nitric oxide (NO), respectively] or anandamide (18.3 +/- 2.2 and 24.3 +/- 3.0 nM, respectively) results in NO release, whereas exposure to the human immunodeficiency virus envelope protei...
journal_title：Journal of cardiovascular pharmacology
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更新日期：1998-06-01 00:00:00
