Ishida Y, Ozaki H, Shibata S
Br J Pharmacol. 1980;71(1):343-8. doi: 10.1111/j.1476-5381.1980.tb10945.x.
1 Caroverine fumarate, 1-(2-diethylaminoethyl)-3-(p-methoxy-benzyl)-1,2-dihydro-2-quinoxalinone fumarate, caused a greater inhibition of the pressor response to KCl (8 x 10(-2) M) than that to noradrenaline (10(-6) M) in the rat hindquarter preparation. 2 In the isolated aorta of the rat, caroverine (up to 10(-6) M) markedly suppressed the contraction caused by KCl (4 x 10(-2) M) (high-K) but had little effect on the contractile response to noradrenaline (10(-6) M) whether added before the spasmogen or in its presence. 3 In the high-K-treated aorta, caroverine shifted the concentration-response curve for external calcium to the right, competitively. The negative logarithm of the affinity (pA2) of caroverine was calculated to be approx. 7. 4 Increased 45Ca uptake of the high-K-treated aorta measured by a modified lanthanum method was inhibited by either caroverine (3 x 10(-6) M) or verapamil (10(-6) M). 5 Concentrations of caroverine and verapamil reducing high-K-induced aortic contraction to 50% of its maximum were 2.4 x 10(-7) and 6.6 x 10(-8) M respectively. 6 Following washout the caroverine-induced inhibition of high-K-induced aortic contraction was more rapidly restored than the verapamil-induced inhibition. 7 These results suggest that caroverine fumarate is a specific and readily reversible calcium influx inhibitor in the rat vascular smooth muscle.
1 富马酸卡罗维林，即1-(2-二乙氨基乙基)-3-(对甲氧基苄基)-1,2-二氢-2-喹喔啉酮富马酸盐，在大鼠后肢制备实验中，对氯化钾（8×10⁻² M）所致升压反应的抑制作用比对去甲肾上腺素（10⁻⁶ M）所致升压反应的抑制作用更强。2 在大鼠离体主动脉实验中，卡罗维林（浓度高达10⁻⁶ M）能显著抑制氯化钾（4×10⁻² M）（高钾）引起的收缩，但对去甲肾上腺素（10⁻⁶ M）引起的收缩反应影响很小，无论在致痉剂之前添加还是在其存在时添加。3 在高钾处理的主动脉中，卡罗维林能竞争性地使细胞外钙的浓度-反应曲线右移。卡罗维林的亲和力负对数（pA2）经计算约为7。4 用改良镧法测定的高钾处理主动脉中45Ca摄取量的增加，被卡罗维林（3×10⁻⁶ M）或维拉帕米（10⁻⁶ M）抑制。5 使高钾诱导的主动脉收缩降低至其最大值50%的卡罗维林和维拉帕米浓度分别为2.4×10⁻⁷ M和6.6×10⁻⁸ M。6 洗脱后，卡罗维林诱导的高钾诱导主动脉收缩抑制作用的恢复比维拉帕米诱导的抑制作用恢复得更快。7 这些结果表明，富马酸卡罗维林是大鼠血管平滑肌中一种特异性且易于逆转的钙内流抑制剂。
