Sanz C, Cortijo J, Perpiñá M, Esplugues J, Morcillo E J
Departamento de Farmacología, Facultad de Medicina, Universidad de Valencia y Alcalá de Henares, Spain.
J Pharm Pharmacol. 1988 Feb;40(2):120-5. doi: 10.1111/j.2042-7158.1988.tb05194.x.
There is increasing interest in the therapeutic potential of calcium antagonists in asthma. Among them the use of calmodulin antagonists deserves consideration. In the present work the effect of trifluoperazine on contractions generated by different mechanisms (CaCl2, KCl, acetylcholine, histamine and 5-hydroxytryptamine) in lung parenchyma strip isolated from control and actively sensitized guinea-pigs has been studied. Trifluoperazine produced both in unsensitized and sensitized lung strips, a concentration-dependent, right, downward displacement of the concentration-response curves to the agonists used, although the sensitization procedure resulted in a potentiation in the ability of trifluoperazine to inhibit agonist-induced contractions. The basis for this greater potency of trifluoperazine in sensitized tissues remains to be elucidated but raises attention to the future use of selective calmodulin antagonists in the management of asthma.
钙拮抗剂在哮喘治疗方面的潜在作用正受到越来越多的关注。其中，钙调蛋白拮抗剂的应用值得考虑。在本研究中，我们研究了三氟拉嗪对从对照和主动致敏豚鼠分离的肺实质条带中由不同机制（氯化钙、氯化钾、乙酰胆碱、组胺和5-羟色胺）引发的收缩的影响。三氟拉嗪在未致敏和致敏的肺条带中，均使所用激动剂的浓度-反应曲线发生浓度依赖性的、向右下方的位移，尽管致敏过程增强了三氟拉嗪抑制激动剂诱导收缩的能力。三氟拉嗪在致敏组织中效力更强的原因仍有待阐明，但这引起了人们对选择性钙调蛋白拮抗剂未来在哮喘治疗中应用的关注。
