内皮素-1（ET-1）和内皮素-3（ET-3）对惊厥发作的影响。

Effects of endothelin-1 (ET-1) and endothelin-3 (ET-3) on convulsive seizures.

作者信息

Getova D P, Maslarova J E, Nikolov R K, Semkova I S

机构信息

Department of Experimental Pharmacology, Medical University Plovdiv, Bulgaria.

出版信息

Methods Find Exp Clin Pharmacol. 1994 Apr;16(3):173-8.

PMID:8046950

Abstract

Endothelins (ET-1 and ET-3) are produced in the brain and may act as neuropeptides. The effects of two endothelins (ET-1 and ET-3) were investigated using pentylenetetrazole- (PTZ), strychnine- (STR), picrotoxin- (PIC) and bicuculline-induced (BIC) convulsions. ET-1 did not exert any anticonvulsive effect. ET-3, being more specific for the brain, showed anticonvulsive activity on PTZ and BIC seizures, but not on PIC and STR seizures. Different mechanisms underlie the action of the convulsants. PTZ, BIC and PIC realized their convulsive effects through the GABAergic inhibitory transmitter system; STR exerted an excitatory effect on the spinal cord by blocking the glycine transmitter system. The results suggest that the anticonvulsive effects of ET-3 might be due to an indirect influence on the GABAergic system in the brain.

摘要

内皮素（ET - 1和ET - 3）在大脑中产生，可能作为神经肽发挥作用。使用戊四氮（PTZ）、士的宁（STR）、印防己毒素（PIC）和荷包牡丹碱诱导（BIC）惊厥来研究两种内皮素（ET - 1和ET - 3）的作用。ET - 1未发挥任何抗惊厥作用。ET - 3对大脑更具特异性，对PTZ和BIC诱导的惊厥显示出抗惊厥活性，但对PIC和STR诱导的惊厥则没有作用。不同的惊厥剂作用机制不同。PTZ、BIC和PIC通过GABA能抑制性递质系统实现其惊厥作用；STR通过阻断甘氨酸递质系统对脊髓产生兴奋作用。结果表明，ET - 3的抗惊厥作用可能是由于对大脑中GABA能系统的间接影响。