Wirkungen von Cyclandelat auf das ZNS — Eine doppelblinde,placebo-kontrollierte Studie an gesunden Probanden

Summary The effect of cyclandelate (Natil^®) on the CNS was tested in a double-blind, placebocontrolled pilot study on 48 healthy males using a single oral dosage of 1200 mg. The EEG was evaluated quantitatively by spectral analysis before and one hour as well as two and a half hours after drug or placebo administration under resting conditions and while performing a test of mental arithmetics. Under resting conditions the power in the alpha₂ frequency band of the signals from the frontal and central recordings was increased in the cyclandelate group in comparison to the placebo group. This effect was still observed two and a half hours after drug intake.Under the condition of mental arithmetics no drug related effect was observed in the EEG. The cyclandelate induced increase of spectral power in the alpha₂ frequency band under resting conditions demonstrates a general effect of cyclandelate on the CNS. The results are discussed with respect to the known age related decrease of spectral power in the alpha frequency band. The established effect of cyclandelate in young healthy subjects calls for a study with chronic treatment in elderly subjects or patients with cognitive deficits.

     

Action of cyclandelate on the development of collateral vessels in the rabbit

Summary

The development of collateral vessels after ligation of the external iliac artery and the femoral artery was studied in the rabbit. ‘Plastoid’ casts of the vascular system showed that daily oral administration of cyclandelate in doses of 100 or 250?mg./kg. accelerated the normal physiological development of the collateral vessels in a region with vascular insufficiency.

It is postulated that promotion of collateral vessel formation is one of the major actions of cyclandelate in peripheral vascular insufficiency when this condition is not based on vascular spasm. Where spasms are involved, the spasmolytic activity of cyclandelate plays a role in its therapeutic effect.     

3.3.5-三甲基环己醇酯类的合成

为了寻找扩张脑血管的新药,本文用D(-)-(?)-氨基丁醇将(±)-(?)羟基苯乙酸(扁桃酸)拆分成左、右旋对映体,再分别与顺式3.3.5-三甲基环已醇酯化,制得二个有旋光性的环扁批酸酯(Ⅵ,Ⅶ);此外,还合成了与它们相应的菸酸酯盐酸盐(Ⅷ,Ⅸ)及安妥明酸酯(Ⅹ,Ⅺ)。 (±)环扁桃酸酯的安妥明酸酯(Ⅲ)、丙酸酯(Ⅳ)及2-甲基丙酸酯(Ⅴ)、3.3.5-三甲基环已醇的顺反异构体的3.4-二甲氧基苯甲酸酯(ⅩⅢ、ⅪⅤ)和3.4.5-三甲氧基苯甲酸酯(ⅩⅤ.ⅩⅥ)也分别被合成。     

环扁桃酯与菸酸环扁桃酯的药理比较研究

静脉注射环扁桃酯与菸酸环扁桃酯对麻醉狗内颈动脉灌注压、股动脉血压皆有降低作用。在低剂量时菸酸环扁桃酯作用比环扁桃酯强,大剂量则作用不如环扁桃酯强。二药皆可显著增加离体免心的冠脉流量和对抗BaCl_2对冠脉的收缩作用以及解除乙酰胆碱引起豚鼠离体回肠的强直收缩作用,但环扁桃酯作用比菸酸环扁桃酯强。静脉注射小鼠LD_(50)表明,菸酸环扁桃酯毒性较低,但腹腔注射毒性比环扁桃酯高。     

环扁桃酯对大鼠血液流变性及血栓形成的影响

目的研究环扁桃酯对血流变和血栓形成的影响。方法测定环扁桃酯高、低剂量组大鼠的全血粘度、血小板聚集率、红细胞压积、血栓湿重,并与正常对照组、阿司匹林组进行比较。结果环扁桃酯的高剂量组降低全血粘度的效果最显著,高切变率80s~(-1)降低率为19．5％,低切变率20s~(-1)降低率为26．2％;环扁桃酯的高剂量组使血小扳聚集率明显降低,最大聚集率下降了29．2％;与空白对照组比较,环扁桃酯高剂量组使血栓湿重明显降低。结论提示环扁桃酯是改善血流变及血栓形成的有效药物。