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麻醉猫静注二甲基哌啶乙胍(BD-38)1～5mg/kg或十二指肠内注入10mg/kg,麻醉狗静注5mg/kg,均引起血压显著下降,心电图无明显的改变。 BD-38部分抑制电刺激离体豚鼠回肠壁的收缩;显著地阻断电刺激动脉周围神经引起的回肠抑制性(松弛)反应。BD-38可明显地抑制电刺激猫内脏神经离中端所引起的升压。清醒猫静脉注射胍乙啶和BD-38(5或10mg/kg)引起瞬膜松弛的作用强度相同。清醒猫灌胃给胍乙啶和BD-38(10mg/kg),胍乙啶的瞬膜松弛作用强度只有BD-38的一半,增加剂量至20mg/kg,才达到BD-38组的松弛程度,说明BD-38胃肠道吸收较胍乙啶为优。 电刺激猫迷走神经外周端引起的降压和心率变慢,给BD-38后稍有阻断,1/2小时内恢复。对乙酰胆硷的作用无明显改变。BD-38也能抑制因阻断颈总动脉引起的加压反射。 离体豚鼠心肺标本,血中BD-38浓度为0.25mg/ml,对心率、心输出量无改变,浓度增至2mg/ml,也不抑制心脏。BD-38不影响洋地黄毒甙的毒性。 狗亚急性毒性试验,未发现对生长和肝功能的影响。BD-38具有持久的降压效果、胃肠道吸收良好、静注无急性拟交感反应、对心脏无直接抑制作用,值得临床试用。
Anesthetic dogs intravenous injection of dimethylpipeididine (BD-38) 1 ~ 5mg / kg or intraduodenal injection of 10mg / kg, intravenous anesthesia dogs 5mg / kg, were caused by a significant drop in blood pressure, ECG was no significant change. BD-38 partially inhibits the electrical stimulation of contractile contraction of the guinea pig ileum wall; significantly blocks the ileal suppressive (relaxation) response induced by electrical stimulation of the peripheral nerves of the artery. BD-38 significantly inhibited the step-up induced by electrical stimulation of the visceral nerves from the midpoint. Conscious cats intravenous guanethidine and BD-38 (5 or 10mg / kg) caused the same effect on the relaxation of the instantaneous membrane. In the awake cats, guanidine and BD-38 (10 mg / kg) were administered intragastrically in guinea pigs. The guanidine edema was only half as strong as that of BD-38, and the dosage was only 20 mg / kg to achieve relaxation of BD-38 , Indicating that BD-38 gastrointestinal absorption than guanethidine is better. The antihypertensive and heart rate changes induced by electrical stimulation of the vagus nerve at the peripheral end of the cats were slowed to a slight extent after BD-38 and resumed within 1/2 hour. The role of acetylcholine no significant change. BD-38 also inhibits baroreflex caused by blocking the common carotid artery. Isolated guinea pig heart and lung specimens, blood BD-38 concentration of 0.25mg / ml, no change in heart rate, cardiac output, the concentration increased to 2mg / ml, does not inhibit the heart. BD-38 does not affect the toxicity of digitalis glycosides. Subacute acute toxicity test in dogs, found no effect on growth and liver function. BD-38 has a long-lasting antihypertensive effect, good gastrointestinal absorption, intravenous injection without acute sympathetic response, no direct inhibition of the heart, it is worth clinical trial.