Machová J, Bauer V, Bilcíková L
Institute of Experimental Pharmacology, Centre of Physiological Sciences, Slovak Academy of Sciences, Bratislava, Czechoslovakia.
Eur J Pharmacol. 1989 Mar 29;162(3):387-95. doi: 10.1016/0014-2999(89)90329-4.
Vincamine in low concentrations induced a sustained contraction of the isolated guinea pig trachealis with long latency and slow onset and, in high concentrations, it induced relaxation which was potentiated in the precontracted trachealis. Vinpocetine had actions similar to those of vincamine on trachealis, however its relaxant effect was more pronounced. The vincamine-induced trachealis contraction was not changed by substance P desensitization, was reduced by tetrodotoxin, nifedipine and low Ca2+ high Mg2+ solution and increased in nominally Ca2+-free solution. The vincamine-induced relaxation of precontracted trachealis was increased by guanethidine and was not affected by propranolol, high Mg2+-low Ca2+ solution and tetrodotoxin. Vincamine- and vinpocetine-induced trachealis contraction as well as vinpocetine-induced relaxation at basal tension were abolished by indomethacin. Vincamine in a low concentration shifted to the left the concentration-effect curve for CaCl2 in the K+-depolarized trachealis, and shifted it to the right at a high concentration. Our results indicate that the contractile and relaxant actions of vincamine and vinpocetine on the guinea pig trachealis may be due to the generation of prostaglandins and to changes in the membrane Ca2+ fluxes and/or the intracellular Ca2+ distribution.
低浓度长春胺可引起豚鼠离体气管平滑肌持续收缩,潜伏期长且起效缓慢;高浓度时则引起舒张,且在预收缩的气管中这种舒张作用增强。长春西汀对气管平滑肌的作用与长春胺相似,但其舒张作用更显著。长春胺诱导的气管收缩不受P物质脱敏的影响,可被河豚毒素、硝苯地平和低钙高镁溶液减弱,在无钙溶液中增强。长春胺诱导的预收缩气管舒张可被胍乙啶增强,不受普萘洛尔、高镁低钙溶液和河豚毒素的影响。吲哚美辛可消除长春胺和长春西汀诱导的气管收缩以及长春西汀在基础张力下诱导的舒张。低浓度长春胺可使K⁺去极化的气管中氯化钙的浓度-效应曲线左移,高浓度时则使其右移。我们的结果表明,长春胺和长春西汀对豚鼠气管的收缩和舒张作用可能是由于前列腺素的生成以及膜Ca²⁺通量和/或细胞内Ca²⁺分布的变化。