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Specific binding sites of platelet activating factor on the intact bovine cerebral microvascular endothelial cells and antagonism of drugs

   
@article{APS6223,
	author = {Du-Xing Sun and Yao-Cheng Rui and Guo-Qian Zeng and Ju Zhu and You-An Shen},
	title = {Specific binding sites of platelet activating factor on the intact bovine cerebral microvascular endothelial cells and antagonism of drugs},
	journal = {Acta Pharmacologica Sinica},
	volume = {13},
	number = {4},
	year = {2016},
	keywords = {},
	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.},
	issn = {1745-7254},	url = {http://www.chinaphar.com/article/view/6223}
}