5α-孕烷-3α-醇-20-酮可阻断尼古丁诱发的癫痫发作并增强双脉冲抑制。
5 alpha-Pregnan-3 alpha-ol-20-one blocks nicotine-induced seizures and enhances paired-pulse inhibition.
作者信息
Luntz-Leybman V, Freund R K, Collins A C
机构信息
Institute for Behavioral Genetics, University of Colorado, Boulder 80309.
出版信息
Eur J Pharmacol. 1990 Aug 28;185(2-3):239-42. doi: 10.1016/0014-2999(90)90648-p.
5 alpha-Pregnan-3 alpha-ol-20-one (3 alpha-OH-DHP) blocked seizures induced by nicotine (4 mg/kg, i.p.) in C3H male mice with an ID50 of 2.37 +/- 0.66 mg/kg (average +/- 95% confidence limit). This steroid (1 microM) also increased paired-pulse inhibition in the hippocampus approximately 40% after 50 min exposure; nicotine (200 microM) partially reversed this effect. Since nicotine and 3 alpha-OH-DHP may have opposite effects on endogenous inhibitory systems, it is proposed that nicotine-induced seizures may involve a disinhibitory mechanism and that 3 alpha-OH-DHP protects against seizures by preventing disinhibition.
5α-孕烷-3α-醇-20-酮（3α-OH-DHP）可阻断C3H雄性小鼠中由尼古丁（4mg/kg，腹腔注射）诱导的癫痫发作，半数抑制剂量（ID50）为2.37±0.66mg/kg（平均值±95%置信限）。在暴露50分钟后，这种类固醇（1μM）还可使海马体中的双脉冲抑制增加约40%；尼古丁（200μM）可部分逆转这种作用。由于尼古丁和3α-OH-DHP可能对内源性抑制系统产生相反的作用，因此有人提出，尼古丁诱导的癫痫发作可能涉及去抑制机制，而3α-OH-DHP通过防止去抑制来预防癫痫发作。
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