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首页> 外文OA文献 >Comparison of the airways relaxant and hypotensive potencies of the potassium channel activators BRL 55834 and levcromakalim (BRL 38227) in vivo in guinea-pigs and rats.
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Comparison of the airways relaxant and hypotensive potencies of the potassium channel activators BRL 55834 and levcromakalim (BRL 38227) in vivo in guinea-pigs and rats.

机译：豚鼠和大鼠体内钾通道激活剂BRL 55834和levcromakalim（BRL 38227）的气道舒张和降压效能的比较。

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1. BRL 55834, a novel potassium channel activator, has been compared with levcromakalim (BRL 38227) for its relaxant effects in vivo on the airways and vasculature of the guinea-pig and rat. 2. When administered intravenously 2 min prior to challenge, BRL 55834 and levcromakalim each inhibited histamine-induced increases in airways resistance (Raw) in the anaesthetized guinea-pig, with BRL 55834 showing a 4.5 fold greater potency than levcromakalim (ED25 = 2.5 micrograms kg-1 and 11.3 micrograms kg-1 respectively). By contrast, both compounds had similar hypotensive potencies (ED18 = 8.5 micrograms kg-1 and 6.5 micrograms kg-1 respectively). 3. In the same guinea-pig model, intraduodenally administered BRL 55834 (100 and 250 micrograms kg-1) and levcromakalim (500 micrograms kg-1) each protected against histamine-induced changes in Raw and dynamic lung compliance (Cdyn), both compounds showing a rapid onset of action that persisted for more than 50 min. The lower dose of BRL 55834 had a similar bronchodilator effect to that of levcromakalim, yet both doses of BRL 55834 elicited substantially smaller effects than levcromakalim on mean arterial blood pressure. 4. In the anaesthetized rat, BRL 55834 and levcromakalim each evoked a dose-related inhibition of inhaled methacholine-induced changes in Raw and Cdyn when given i.v., with BRL 55834 showing some four fold greater potency than levcromakalim (BRL 55834: Raw ED35 = 3.7 micrograms kg-1, Cdyn ED35 = 5.9 micrograms kg-1; levcromakalim: Raw ED35 = 16 micrograms kg-1, Cdyn ED35 = 23.5 micrograms kg-1).(ABSTRACT TRUNCATED AT 250 WORDS)
机译：1.一种新型的钾通道激活剂BRL 55834已与左旋可卡林（BRL 38227）在体内对豚鼠和大鼠的气道和脉管系统具有松弛作用，已进行了比较。 2.在激发前2分钟静脉内给药时，BRL 55834和左旋克马卡林各自抑制了组胺诱导的麻醉豚鼠的气道阻力（Raw）增加，其中BRL 55834的效力比左旋克罗卡林（ED25 = 2.5微克）高4.5倍。 kg-1和11.3微克kg-1）。相比之下，两种化合物都具有相似的降压潜能（ED18分别为8.5微克kg-1和6.5微克kg-1）。 3.在相同的豚鼠模型中，十二指肠内分别施用BRL 55834（100和250微克kg-1）和左旋克罗卡林（500微克kg-1）可防止组胺引起的生和动态肺顺应性（Cdyn）变化，两者化合物显示起效迅速，持续时间超过50分钟。较低剂量的BRL 55834具有与左旋卡马林相似的支气管扩张剂作用，但两种剂量的BRL 55834引起的平均动脉血压的作用均远小于左旋马卡林。 4.在麻醉的大鼠中，静脉给予BRL 55834和levcromakalim均引起剂量相关的吸入性甲胆碱诱导的Raw和Cdyn改变的剂量抑制，BRL 55834显示的效力比levcromakalim大四倍（BRL 55834：Raw ED35 = 3.7微克kg-1，Cdyn ED35 = 5.9微克kg-1;左旋克马林：原始ED35 = 16微克kg-1，Cdyn ED35 = 23.5微克kg-1）（摘要截断为250个字）

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