Raeburn D, Rodger I W
Br J Pharmacol. 1984 Oct;83(2):499-504. doi: 10.1111/j.1476-5381.1984.tb16513.x.
The effects of verapamil on leukotriene D4 (LTD4)- and KCl-induced contractions and 45Ca-uptake were examined in guinea-pig isolated tracheal smooth muscle. Both LTD4 (0.1 to 200 nmol l-1) and KCl (8 to 125 mmol l-1) produced concentration-dependent increases in tension in the tracheal preparations. Verapamil (1 mumol l-1) inhibited the tension responses induced by both LTD4 and KCl. LTD4 failed to increase the lanthanum-resistant Ca content of tracheal smooth muscle at either low (EC25; 3 nmol l-1) or high (EC90; 50 nmol l-1) concentrations. Verapamil did not modify this result. KCl (90 mmol l-1) increased the lanthanum-resistant Ca content of the smooth muscle by approximately 60% over basal levels. This effect was completely inhibited by verapamil (1 mumol l-1). It is concluded that in this tissue, LTD4 utilizes principally an intracellular source of Ca2+ to initiate contraction whereas KCl is dependent upon the uptake of Ca2+ from the extracellular compartment. It is suggested that the inhibitory effects of verapamil may reflect an intracellular mechanism of action directed against Ca2+ release initiated by LTD4.
在豚鼠离体气管平滑肌中研究了维拉帕米对白三烯D4(LTD4)和氯化钾诱导的收缩以及45钙摄取的影响。LTD4(0.1至200纳摩尔/升)和氯化钾(8至125毫摩尔/升)均使气管标本中的张力呈浓度依赖性增加。维拉帕米(1微摩尔/升)抑制了LTD4和氯化钾诱导的张力反应。LTD4在低浓度(EC25;3纳摩尔/升)或高浓度(EC90;50纳摩尔/升)时均未能增加气管平滑肌中镧抗性钙含量。维拉帕米未改变这一结果。氯化钾(90毫摩尔/升)使平滑肌中镧抗性钙含量比基础水平增加约60%。维拉帕米(1微摩尔/升)完全抑制了这一效应。得出的结论是,在该组织中,LTD4主要利用细胞内钙源引发收缩,而氯化钾则依赖于从细胞外区摄取钙。提示维拉帕米的抑制作用可能反映了针对LTD4引发的钙释放的细胞内作用机制。