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顺—3,4—二氯—α—氯代桂皮酰另丁胺(代号:8601)为一种新的桂皮酰胺类化合物。它对MES有很强的对抗作用,其EK_(50)为20.3mg/kg,明显强于抗痫灵(ED_(50)为88.5mg/kg)。前者的治疗指数>44.3,后者为6.3。所以,8601有可能成为一种作用强、安全范围大的新的抗癫痫药。它也能有效的对抗icv谷氨酸钠和ZnSO_4所引起的惊厥,但对士的宁惊厥则无明显影响。8601抗最大抗电休克发作试验作用的机制可能与其升高脑中5HT和降低中枢兴奋性神经递质Glu和AsP的含量有关。
Cis-3,4-dichloro-α-chlorocinnamylbutylamine (Code: 8601) is a new cinnamide compound. It has a strong antagonistic effect on MES with an EK 50 of 20.3 mg / kg, which is significantly stronger than that of anti-epilepsy (ED 50) at 88.5 mg / kg. The former’s therapeutic index was> 44.3, while the latter was 6.3. So, 8601 is likely to become a new type of antiepileptic drug with a strong and safe range. It is also effective against icv monosodium glutamate and ZnSO_4-induced convulsions, but does not have a significant effect on strychnine-induced convulsions. The mechanism of the 8601 anti-maximal anti-shock test may be related to increasing 5HT in the brain and decreasing the levels of central excitatory neurotransmitters Glu and AsP.