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用放射配体受体结合分析法,观察了三氯乙醇(TCEt)对5-HT3受体激动剂5-HT和5-HT3受体拮抗剂ICS205-930与[3H]BRL16170竞争大鼠脑皮质5-HT3受体能力的影响。结果证实,TCEt(4mmol·L-1)能使5-HT竞争受体的浓度-反应曲线左移,半数抑制结合浓度降低(P<0.01),斜率无显著改变;而对ICS205-93O未见明显影响。表明TCEt能增强5-HT与5-HT3受体结合的能力,提示它可能通过这一机制促进5-HT3配体闸门离子通道开放而发挥作用。
Radioligand binding assay was used to observe the effects of trichloroethanol (TCEt) on rat brain cortex competition with 5-HT3 receptor agonist 5-HT and 5-HT3 receptor antagonist ICS205-930 and [3H] BRL16170 5-HT3 receptor capacity. The results showed that TCEt (4mmol·L-1) shifted the concentration-response curve of 5-HT competing receptor to the left and the half inhibitory concentration decreased (P <0.01), while the slope of ICS205-93O No obvious effect. The results showed that TCEt could enhance the binding of 5-HT to 5-HT3 receptor, suggesting that TCEt may play a role in promoting the opening of 5-HT3 ligand gate channel by this mechanism.