论文部分内容阅读
小白鼠腹腔注射胍乙哌啶、BD-37、BD-38、胍乙啶和BD-31的LD_(50)分别为367,243,202,155和78 mg/kg。麻醉大白鼠和猫静脉注射胍乙啶、胍乙哌啶和BD-37出现血压短暂下降继而升压,然后再下降,而BD-38和BD-31仅有降压作用。急性降压强度BD-38和BD-31较强,BD-37和胍乙啶次之,胍乙哌啶最弱。胍乙啶、胍乙哌啶、BD-37和BD-31抑制酪胺的升压作用;对去甲肾上腺素的升压,除BD-31稍有抑制外,胍乙啶、BD-37和BD-38反有增敏作用。胍乙啶、胍乙哌啶和BD-37明显增强豚鼠心房的收缩,BD-38和BD-31则无此作用。离体豚鼠输精管和猫颈交感神经实验说明,BD-31阻断交感神经节的作用较强,对神经末梢也稍有阻断;BD-37和BD-38阻断交感神经末梢与胍乙啶的作用强度相仿;胍乙哌啶只对输精管稍有阻断作用。胍乙啶、胍乙哌啶、BD-37和BD-38可减低大鼠心脏内去甲肾上腺素的含量,BD-31未见减低。 以上结果表明:BD-38能选择地阻断交感神经末梢,而无胍乙啶的交感类似反应,并具有较强的降压效果。
The LD50 of BD-37, BD-38, guanethidine and BD-31 were 367, 243, 202, 155 and 78 mg / kg, respectively. In anesthetized rats and cats, intravenous administration of guanethidine, guanidine, and BD-37 resulted in a brief decrease in blood pressure followed by a step-up and then decrease of BD-38 and BD-31 with only a hypotensive effect. BD-38 and BD-31 were stronger in acute antihypertensive intensity, followed by BD-37 and guanethidine, and guanidine eprineridine was the weakest. Guanidine, guanethidine, BD-37 and BD-31 inhibited the tyramine’s step-up effect. For norepinephrine boosted, except for BD-31, guanidine, BD-37 and BD-38 anti-sensitization. Guanidine, guanethidine and BD-37 significantly enhanced the atrial contraction in guinea pigs, but BD-38 and BD-31 did not. Ex vivo guinea pig vas deferens and cat neck sympathetic nerve experiments show that, BD-31 block sympathetic ganglia strong role in nerve endings also slightly blocked; BD-37 and BD-38 block sympathetic nerve end and guanethidine The effect of similar intensity; Guanidine Etanercept only slightly blocked the role of the vas deferens. Guanidine, guanethidine, BD-37 and BD-38 decreased the content of norepinephrine in rat’s heart, while BD-31 showed no decrease. The above results show that: BD-38 can selectively block the sympathetic nerve endings, but without guanethidine sympathetic similar reactions, and has a strong antihypertensive effect.