豚鼠肺膜LTD4受体结合特征及二苯乙烯低聚体(Gn-3)的LTD4受体拮抗作用

侯艳宁 朱秀媛 程桂芳

中国药学杂志 ›› 2000, Vol. 35 ›› Issue (10) : 667-669.

中国药学杂志
中国药学杂志 ›› 2000, Vol. 35 ›› Issue (10) : 667-669.
药理

豚鼠肺膜LTD4受体结合特征及二苯乙烯低聚体(Gn-3)的LTD4受体拮抗作用

  • 侯艳宁，朱秀媛，程桂芳
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Studies on the characteristics of LTD4receptor with radio-ligand binding assay and the effect of Gn-3

  • HOU Yan-ning,ZHU Xiu-yuan,CHENG Gui-fang
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摘要

目的 采用LTD4放射受体结合实验方法，在分析LTD4受体的有关特征的基础上，观察比较二苯乙烯低聚体(Gn-3)对LTD4受体的拮抗作用。方法 以豚鼠肺膜为实验材料，采用3H-LTD4为放射配体，以FPL55712作阳性对照药物，Gn-3为实验药物，进行药物竞争结合实验。采用离体器官生物检测法鉴定Gn-3对LTD4受体的拮抗作用。结果3H-LTD4与其相应受体呈现单一结合位点，其Kd和Bmax值分别为19.9×10-11mol·L-1和232.9 fmol·mg-1蛋白。Gn-3可明显取代3H-LTD4与其受体结合，IC50值为5.71×10-7 mol·L-1，Ki值为2.54×10-7 mol·L-1。生物学鉴定法证实Gn-3可抑制LTD-4引起的生物学效应。结论 豚鼠肺膜LTD4受体为单一结合位点受体，Gn-3为高活性的LTD4受体拮抗剂。

Abstract

OBJECTIVE To study the effect of Gn-3 on the LTD4receptor by using a radio-ligand binding assay of LTD4. METHODS Lung membrane of guinea pig was used as experimental materials,3H-LTD was used as radio ligand,FPL55712was chosen as the positive control drug,Gn-3 was used as the tested drug and bioassay in vitro was used to determine the biological function of Gn-3. RESULTS The binding of 3H-LTD 4 to its receptor was specific,saturable and reversible.The Kd and Bmaxvalues were 19.9×10-11mol·L-1and 232.9 fmol·mg-1 protein respectively at 30℃.Gn-3 inhibited 3H-LTD4in competing against LTD4receptor.The IC50and Ki value were 5.71×10-7mol·L-1and 2.54×10-7mol·L-1respectively.It was also determined that Gn-3 was LTD4 receptor antagonist by the bioassay in vitro. CONCLUSION The binding of 3H-LTD4on guinea pig lung membrane showed a single binding site.Gn-3 appeared to be an effective LTD4 receptor antagonist.

关键词

LTD4 / 放射受体结合 / 拮抗剂 / 二苯乙烯低聚体

Key words

LTD4 / radioreceptor assay / antagonist / Gn-3

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侯艳宁 朱秀媛 程桂芳. 豚鼠肺膜LTD4受体结合特征及二苯乙烯低聚体(Gn-3)的LTD4受体拮抗作用[J]. 中国药学杂志, 2000, 35(10): 667-669
HOU Yn-ning;ZHU Xiu-yun;CHENG Gui-fng. Studies on the characteristics of LTD4receptor with radio-ligand binding assay and the effect of Gn-3[J]. Chinese Pharmaceutical Journal, 2000, 35(10): 667-669

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