二甲苯胺噻唑神经药理作用的研究

本实验对二甲苯胺噻唑(静松灵)的镇静、镇痛、肌松、安定和抗惊厥等中枢抑制作用进行了较为系统的研究;观察了该药对大鼠自发性脑电变化的影响;对该药的作用机理作了初步探讨。结果:(1)二甲苯胺噻唑具有良好的镇静、镇痛和松肌作用,较大剂量有一定的安定作用,但安全性差;(2)对戍四氮、士的宁和苦味毒所致惊厥反应无对抗作用;(3)对神经于神经冲动的传导具有阻断效应,(4)可诱导大鼠脑电出现高幅慢波,惊醒反应消失,妥拉苏林和育亨宾对此有拮抗作用;(5)妥拉苏林和育亨宾对二甲苯胺噻唑制动大有催醒作用,且可缓解该药的中毒反应。结果提示,中枢性α_2—肾上腺素能受体参与了二甲苯胺噻唑中枢抑制作用的产生过程。

NEUROPHARMACOLOGICAL ACTIONS OF XYLIDINOTHIAZOLE

In the experiment, we have made a systematic study on the neurophar-macological actions of xylidinothiazole and inquired into its mechanisms of depres-sion. The results are summarized as fllows: 1 .The drug has analgesic, sedative andmyorelaxant effects. At larger dose it also has tranquilizing effect but not reliable. 2.The drug could not inhibit convulsion induced by pentylenetetrazol, strychine andpicrotoxin but could decrease mortality caused by them in mice .It was thoughtthat their antagonisms are not specific. 3. It could block the conduction of sciaticnerve impulse in frogs. 4. In unanesthetized rats it produced a high synchronizationand blocked the EEG arousal response. These effects were antagonized by tolazoline and yohimbine. 5. Tolazoline and yohimbine could antagonize depression in-duced by xylidinothiazole in dogs. Tolazoline also reversed adverse reaction causedby high dose of the drug. These results suggest that alpha-2 adrenergic reteptor is,in certain exient, invol ved in the depression induced by xylidinothiazole.