| 三氯乙醇对5－HT和ICS_（205－930）与［~3H］BRL_（46470 |
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| 引用本文： | 陈重阳. 三氯乙醇对5－HT和ICS_（205－930）与［~3H］BRL_（46470[J]. 中国药理学通报, 1995, 0(1) |
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| 作者姓名： | 陈重阳 |
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| 作者单位： | 桂林医学院药理教研室，英国伯明翰大学医学院药理系 |
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| 摘 要： | 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。
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| 关 键 词： | 三氯乙醇，5－羟色胺，ICs＿（205－930），5NT￣3受体，放射配体受体结合测定 |
The effects of trichloroethanol on the competing binding Of 5-HT and ICS_(205-930) for 5-HT_3 receptor in cerebral cortex of rat with ~3H BR(46470) |
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| CHEN Chong-Yang, Barnes N M. The effects of trichloroethanol on the competing binding Of 5-HT and ICS_(205-930) for 5-HT_3 receptor in cerebral cortex of rat with ~3H BR(46470)[J]. Chinese Pharmacological Bulletin, 1995, 0(1) |
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| Authors: | CHEN Chong-Yang Barnes N M |
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| Abstract: | In the present study.we have examined the actions of trichloroethanol(TCEt) on the competing binding of 5-HT(5-HT3 receptor agonist) and ICS205-930(5-HT3receptor antagonist )with[3H]BRL46470(a 5-HT3 antagonist) incerebral cortex of rat. We observed thatTCEtshifted the competing curve of 5-HT lefttoward and reduced the molar concentration of 5- HT to reduce the specific binding by 50%(IC50), but had no effect on that ofICS205-930.indicating that TCEt appears toenhance the ability of 5-HT to bind with 5HT3 receptor and facilitate the open of the ligand-gated ion channels. These results are consisted with the hypothesis that 5-HT3receptor function may contribute to the behavioral pharmacology of alcohols and their related sedative/hypnotic agents. |
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| Keywords: | hydrotraptamine ICS_(205-930) 5-HT_3 receptor radioligand-receptor binding assay |
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