有证据表明，具有钙拮抗剂特性的药物地尔硫䓬不具有β-肾上腺素受体阻断活性。
Evidence against beta-adrenoceptor blocking activity of diltiazem, a drug with calcium antagonist properties.
作者信息
Briley M, Cavero I, Langer S Z, Roach A G
出版信息
Br J Pharmacol. 1980 Aug;69(4):669-73. doi: 10.1111/j.1476-5381.1980.tb07920.x.
Abstract
1 The isolated spontaneously beating atria of the rat, diltiazem (0.01 to 0.1 microM) shifted the atrial rate concentration-response curves to isoprenaline to the right in a non-parallel manner and depressed their maxima. Under the same experimental conditions, (+/-)-propranolol (0.03 to 0.1 microM) behaved as a competitive beta-adrenoceptor antagonist. 2 Whereas (+/-)-propranolol (IC50 = 12 nM) and isoprenaline (IC50 = 0.9 microM) inhibited (-)-[3H]-dihydroalprenolol binding to rat brain membrane preparations, diltiazem failed to do so in concentrations up to 10 microM. 3 Diltiazem but not (+/-)-propranolol, antagonized the positive chronotropic responses to calcium in spontaneously beating rat atria. 4 It is proposed that diltiazem inhibited the tachycardia induced by isoprenaline through an effect on calcium which may be an essential modulator of the sequence of events linking the beta-adrenoceptor activation and heart rate response.
摘要
- 大鼠离体自发搏动的心房，地尔硫䓬（0.01至0.1微摩尔）以非平行方式使异丙肾上腺素的心房率浓度 - 反应曲线右移，并降低其最大值。在相同实验条件下，（±） - 普萘洛尔（0.03至0.1微摩尔）表现为竞争性β - 肾上腺素能受体拮抗剂。2. 虽然（±） - 普萘洛尔（IC50 = 12纳摩尔）和异丙肾上腺素（IC50 = 0.9微摩尔）抑制（ - ） - [3H] - 二氢阿普洛尔与大鼠脑膜制剂的结合，但地尔硫䓬在浓度高达10微摩尔时未能做到这一点。3. 地尔硫䓬而非（±） - 普萘洛尔，拮抗自发搏动的大鼠心房对钙的正性变时反应。4. 有人提出，地尔硫䓬通过对钙的作用抑制异丙肾上腺素诱导的心动过速，钙可能是连接β - 肾上腺素能受体激活与心率反应的一系列事件的重要调节因子。
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