维拉帕米对大鼠腹膜肥大细胞的双重作用：抑制或诱导组胺释放。

Dual effect of verapamil on rat peritoneal mast cells: inhibition or induction of histamine release.

Lunardi L O, Vugman I

Braz J Med Biol Res. 1982 Oct;15(4-5):269-73.

Abstract

Verapamil (1.0 microM) inhibits histamine release from rat peritoneal mast cells induced by both compound 48/80 (Burroughs Wellcome), an external calcium-independent stimulant, and by protamine, an external calcium-dependent stimulant. 2. The inhibition was reversed by calcium in a concentration-dependent manner and thus seems to be related to the calcium-blocking action of verapamil. The inhibitory effect of 1.0 microM verapamil on protamine-induced histamine release in the presence of 0.5 mM calcium was 64%, and 32% in the presence of 2.0 mM calcium. 3. At concentrations of 0.1-1.0 mM, verapamil induces histamine release. The verapamil-induced release was independent of calcium at lower concentrations but at 1.0 mM, more release was observed in the absence of calcium. Histamine release induced by verapamil was blocked by temperature (2-4 degrees C) and by 2,4-dinitrophenol. Glucose (5 mM) reversed the effect of 2,4-dinitrophenol.

摘要

维拉帕米（1.0微摩尔）可抑制由化合物48/80（必治妥施贵宝公司生产）（一种不依赖细胞外钙的刺激剂）和鱼精蛋白（一种依赖细胞外钙的刺激剂）诱导的大鼠腹膜肥大细胞组胺释放。2. 钙以浓度依赖的方式逆转了这种抑制作用，因此这种抑制作用似乎与维拉帕米的钙阻断作用有关。在存在0.5毫摩尔钙的情况下，1.0微摩尔维拉帕米对鱼精蛋白诱导的组胺释放的抑制作用为64%，在存在2.0毫摩尔钙的情况下为32%。3. 在0.1 - 1.0毫摩尔的浓度下，维拉帕米可诱导组胺释放。维拉帕米诱导的释放在较低浓度下不依赖钙，但在1.0毫摩尔时，在无钙情况下观察到更多的释放。维拉帕米诱导的组胺释放可被温度（2 - 4摄氏度）和2,4 - 二硝基苯酚阻断。葡萄糖（5毫摩尔）可逆转2,4 - 二硝基苯酚的作用。