Cerrina J, Advenier C, Renier A, Floch A, Duroux P
Eur J Pharmacol. 1983 Oct 28;94(3-4):241-9. doi: 10.1016/0014-2999(83)90413-2.
The effects of diltiazem and 3 other Ca2+ antagonists (verapamil, nicardipine, bepridil) were studied on isolated guinea-pig tracheal preparations which were contracted with several agonists. Assessment of the contractile agonists was performed under physiological conditions as well as in Ca2+-depleted solutions. The order of potency of the contractile agonists was LTD4 greater than ACh greater than 5-HT greater than Hist greater than BaCl2 greater than TEA greater than KCl. The efficacy of the physiological agonists ACh, Hist and LTD4 was moderately depressed in Ca2+-free solutions while the responses to non-specific agonists and 5-HT were markedly reduced. Diltiazem and verapamil reduced basal tone at concentrations greater than or equal to 10(-4) M. Diltiazem displaced all agonist concentration-effect curves to the right. The four Ca2+ antagonists studied had a marked effect on non-physiological agonists as compared to that on physiological agents. Increasing Ca2+ concentration only partially reversed the inhibitory effect of diltiazem.
研究了地尔硫䓬和其他3种钙拮抗剂（维拉帕米、尼卡地平、苄普地尔）对用几种激动剂收缩的豚鼠离体气管制备物的作用。在生理条件下以及在缺钙溶液中对收缩性激动剂进行评估。收缩性激动剂的效力顺序为白三烯D4＞乙酰胆碱＞5-羟色胺＞组胺＞氯化钡＞四乙铵＞氯化钾。在无钙溶液中，生理性激动剂乙酰胆碱、组胺和白三烯D4的效力略有降低，而对非特异性激动剂和5-羟色胺的反应则明显减弱。地尔硫䓬和维拉帕米在浓度大于或等于10⁻⁴M时可降低基础张力。地尔硫䓬使所有激动剂浓度-效应曲线右移。与生理性药物相比，所研究的四种钙拮抗剂对非生理性激动剂有显著作用。增加钙浓度只能部分逆转地尔硫䓬的抑制作用。
