Inhibition of bronchoconstriction in the guinea pig by a calcium channel blocker, nifedipine.
Inhibition of bronchoconstriction in the guinea pig by a calcium channel blocker, nifedipine.
复制标题
钙通道阻滞剂硝苯地平抑制豚鼠支气管收缩。
DOI：
10.1164/arrd.1982.125.1.61
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发表时间：
1982
期刊：
影响因子：
--
通讯作者：
Drazen,JM
中科院分区：
文献类型：
--
作者：
Fanta,CH;Venugopalan,CS;Lacouture,PG;Drazen,JM
我们研究了钙通道阻滞剂硝苯地平对豚鼠气道平滑肌收缩的抑制作用。在体外，硝苯地平（0.003 ~ 3.0µM）可引起气管螺旋和实质条内固有张力的显著剂量依赖性逆转。硝苯地平还能抑制两种激动剂组胺和乙醇诱导的气管螺旋和实质条的收缩。在3.0µM的浓度下，硝苯地平使脑实质条最大收缩50%所需的氨基醇浓度增加48倍，组胺浓度增加5倍。增加组织液中细胞外钙离子浓度可显著降低硝苯地平的抑制作用。在体内，硝苯地平（静脉注射30µg/kg体重）没有改变肺阻力或动态顺应性。然而，在研究的5只动物中，它确实减轻了组胺引起的支气管收缩。组胺最大剂量组胺输注后，硝苯地平组肺阻力平均上升40±16% (SEM)，高于对照组的182±65% (p < 0.025)；动态顺应性平均下降35±8%，高于对照组的58±6% （p < 0.01）。因此，这种钙通道阻滞剂抑制介质诱导的中央和周围气道收缩组织的收缩，这一发现具有潜在的临床适用性。
We investigated the inhibitory effects of nifedipine, a calcium channel blocker, on airway smooth muscle constriction in the guinea pig.In vitro, nifedipine (0.003 to 3.0 µM) caused significant dose-dependent reversal of intrinsically existing tone in both tracheal spirals and parenchymal strips. Nifedipine also inhibited the constriction of tracheal spirals and parenchymal strips induced by two different agonists, histamine and carbachol. At a concentration of 3.0 µM, nifedipine increased by 48-fold the concentration of carbachol required to produce a 50% of maximal contraction of parenchymal strips, and by 5-fold the concentration of histamine. Increasing extracellular calcium ion concentration in the tissue baths significantly diminished the inhibitory action of nifedipine.In vivo, nifedipine (30 µg/kg body weight given intravenously) did not alter pulmonary resistance or dynamic compliance. It did, however, attenuate histamine-induced bronchoconstriction in 3 of 5 animals studied. In response to the maximal dose of histamine infused, mean pulmonary resistance rose 40 ± 16% (SEM) after nifedipine versus 182 ± 65% in the control animals (p < 0.025) and mean dynamic compliance decreased 35 ± 8% after nifedipine versus 58 ± 6% in the control animals (p < 0.01). Thus, this calcium channel blocker inhibits mediator-induced constriction of both central and peripheral airway contractile tissues, a finding of potential clinical applicability.