Thorens S, Haeusler G
Eur J Pharmacol. 1979 Feb 15;54(1-2):79-91. doi: 10.1016/0014-2999(79)90410-2.
The "lanthanum method" was used to measure the effects of vasodilators on the 45Ca influx induced in isolated strips of rabbit main pulmonary artery after replacement of NaCl by KCl in the bathing solution. Two Ca antagonists, verapamil and Ro 11-1781, produced dose-dependent inhibitions of 45Ca influx with IC50 values of 3 X 10(-7) and 4 X 10(-6)M, respectively. Papaverine was virtually equipotent with Ro 11-1781 (IC50 = 2 X 10(-6)M). High concentrations of diazoxide (10(-4) to 10(-3)M) and nitroglycerin (10(-3)M) were required to cause inhibitions which did not exceed 40%. While prazosin 3 X 10(-4)M stimulated 45Ca influx, sodium nitrite and sodium nitroprusside had no effect. A comparison of the effects of vasodilators on contraction and 45Ca influx indicated that, of the drugs studied, only Ca antagonists and papaverine may cause relaxation by interfering with Ca influx. While high concentrations (greater than 10(-4)M) of verapamil, papaverine and nitroglycerin produced an inhibition of 45Ca uptake by membrane fractions from rabbit aorta, the other vasodilators tested were inactive.
采用“镧法”测定血管舒张剂对在浴液中用氯化钾替代氯化钠后兔主肺动脉离体条带中诱导的45Ca内流的影响。两种钙拮抗剂维拉帕米和Ro 11-1781对45Ca内流产生剂量依赖性抑制,IC50值分别为3×10(-7)和4×10(-6)M。罂粟碱与Ro 11-1781几乎等效(IC50 = 2×10(-6)M)。需要高浓度的二氮嗪(10(-4)至10(-3)M)和硝酸甘油(10(-3)M)才能产生不超过40%的抑制作用。虽然3×10(-4)M的哌唑嗪刺激45Ca内流,但亚硝酸钠和硝普钠没有作用。血管舒张剂对收缩和45Ca内流影响的比较表明,在所研究的药物中,只有钙拮抗剂和罂粟碱可能通过干扰Ca内流引起舒张。虽然高浓度(大于10(-4)M)的维拉帕米、罂粟碱和硝酸甘油对兔主动脉膜组分的45Ca摄取产生抑制作用,但所测试的其他血管舒张剂没有活性。