当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > 3,8-diazabicyclo--[3.2.1]-octane derivatives as analogues of ambasilide, a Class III antiarrhythmic agent.

3,8-diazabicyclo--[3.2.1]-octane derivatives as analogues of ambasilide, a Class III antiarrhythmic agent.

Abstract：

:Ambasilide, a representative of Class III antiarrhythmics, was reported to prolong the cardiac action potential duration in the dog, with little or no effect on Ca and Na currents. We synthesised a series of ambasilide analogues, having the 3,8-diazabicyclo-[3.2.1]-octane moiety instead of the 3,7-diazabicyclo-[3.3.1]-nonane present in ambasilide. The compounds were tested both in vitro extracellular electrophysiological assays and by the conventional microelectrode technique. Most of them lengthened the effective refractory period (ERP) with no change or slight increase on the impulse conduction time (ICT). Similarly some of the tested compounds lengthened the action potential duration (APD), a typical Class III feature, without exerting any significant effect on the maximal rate of depolarization, therefore apparently lacking Class I antiarrhythmic activity.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Villa S,Barlocco D,Cignarella G,Papp GJ,Baláti B,Takács J,Varró A,Borosy A,Keserû K,Mátyus P

doi

10.1016/s0223-5234(01)01246-6

subject

Has Abstract

pub_date

2001-06-01 00:00:00

pages

495-506

issue

6

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(01)01246-6

journal_volume

36

pub_type

杂志文章

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