| 培养牛脑微血管内皮细胞上血小板激活因子的... |
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| 引用本文： | 孙笃新 芮耀诚. 培养牛脑微血管内皮细胞上血小板激活因子的...[J]. 中国药理学报, 1992, 13(4): 326-329 |
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| 作者姓名： | 孙笃新 芮耀诚 |
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| 摘 要： |
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| 关 键 词： | 血小板 激活因子 药物受体 |
Specific binding sites of platelet activating factor on the intact bovine cerebral microvascular endothelial cells and antagonism of drugs. |
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| D X Sun,Y C Rui,G Q Zeng,J Zhu,Y A Shen. Specific binding sites of platelet activating factor on the intact bovine cerebral microvascular endothelial cells and antagonism of drugs.[J]. Acta Pharmacologica Sinica, 1992, 13(4): 326-329 |
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| Authors: | D X Sun Y C Rui G Q Zeng J Zhu Y A Shen |
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| Affiliation: | Department of Pharmacology, School of Pharmacy, Second Military Medical University, Shanghai, China. |
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| Abstract: | [3H]Triazolodiazepine ([3H]WEB 2086), an antagonist of platelet activating factor (PAF) receptor, was studied as radioligand on intact cerebral microvascular endothelial cells (CMEC). The results showed that the binding of [3H]triazolodiazepine reached and maintained at an equilibrium after 15-120 min of incubation and that it was saturable with increasing concentration of radioligand. Scatchard analysis indicated that there were 2 specific binding sites on CMEC, its Kd1, Bmax1, Kd2, and Bmax2 were 3.13 nmol.L-1, 1.50 pmol/3 x 10(5) cells, 83.96 nmol.L-1, and 12.96 pmol/3 x 10(5) cells, respectively. The binding of [3H]triazolodiazepine to CMEC was displaced by C16-PAF and 1,5-bis-(3,4-dimethoxyphenyl)-tetrahydro-(4H)-pyran (SZ-1), which IC50 were 0.43 nmol.L-1 and 0.125 mumol.L-1, respectively. These data suggested the existence of PAF specific binding sites on CMEC. |
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