论文部分内容阅读
木犀草素(终浓度1.09×10~(-4)M与2.18×10~(-4)M)能明显抑制Schultz-Dale反应。该药对SRS-A引起的豚鼠廻肠收缩有明显的抑制作用,IC_(50)为2.76×10~(-5)M。且可使SRS—A累积量效曲线平行右移,两者呈竞争性拮抗,Lut—SRS—A的PA_2值为4.72。本药对H引起的豚鼠廻肠收缩亦有明显的抑制作用,但累积量效曲线表明为非竞争性拮抗。本药亦可剂量依赖性地抑制电刺激引起的大鼠输精管收缩,但这种作用不是通过竞争性地拮抗(?)·R或激动(?)_2·R,而是直接的解痉作用。由此表明,木犀草素抑制Schultz—Dale反应可能与其竞争性拮抗SRS—A和直接的解痉作用有关。
Luteolin (final concentration 1.09×10 -4 M and 2.18×10 -4 M) significantly inhibited the Schultz-Dale reaction. The drug had a significant inhibitory effect on SRS-A induced guinea pig calf contraction, IC_(50) was 2.76×10~(-5)M. And the cumulative dose-response curve of SRS-A can be shifted to the right and the two are competitively antagonistic. The PA 2 value of Lut-SRS-A is 4.72. The drug also had a significant inhibitory effect on H-induced calf contraction in guinea pigs, but the cumulative dose-response curve showed non-competitive antagonism. The drug can also inhibit the contraction of rat vas deferens induced by electrical stimulation in a dose-dependent manner, but this effect is not through competitive antagonism of (?)R or agonism(?)_2R, but a direct spasmolysis effect. This suggests that the inhibition of the Schultz-Dale response by luteolin may be related to its competitive antagonism of SRS-A and direct spasmolysis.