Fanta C H, Venugopalan C S, Lacouture P G, Drazen J M
Am Rev Respir Dis. 1982 Jan;125(1):61-6. doi: 10.1164/arrd.1982.125.1.61.
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 microM) 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 microM, 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 micrograms/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 less than 0.025) and mean dynamic compliance decreased 35 +/- 8% after nifedipine versus 58 +/- 6% in the control animals (p less than 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.
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至3.0微摩尔)可使气管螺旋条和实质条中原本存在的张力发生显著的剂量依赖性逆转。硝苯地平还可抑制由组胺和卡巴胆碱这两种不同激动剂诱导的气管螺旋条和实质条的收缩。在浓度为3.0微摩尔时,硝苯地平使实质条产生最大收缩50%所需的卡巴胆碱浓度增加了48倍,使组胺浓度增加了5倍。增加组织浴中的细胞外钙离子浓度可显著减弱硝苯地平的抑制作用。在体内,硝苯地平(静脉注射30微克/千克体重)并未改变肺阻力或动态顺应性。然而,在研究的5只动物中有3只,它确实减轻了组胺诱导的支气管收缩。在输注组胺最大剂量后,硝苯地平组平均肺阻力上升40±16%(标准误),而对照组动物为182±65%(p<0.025);硝苯地平组平均动态顺应性下降35±8%,而对照组动物为58±6%(p<0.01)。因此,这种钙通道阻滞剂可抑制介质诱导的中央和外周气道收缩组织的收缩,这一发现具有潜在的临床应用价值。