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Specific binding sites of platelet activating factor on the intact bovine cerebral microvascular endothelial cells and antagonism of drugs.
Zhongguo Yao Li Xue Bao. 1992 Jul; 13(4):326-9.ZY

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.

Authors+Show Affiliations

Department of Pharmacology, School of Pharmacy, Second Military Medical University, Shanghai, China.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

1333718

Citation

Sun, D X., et al. "Specific Binding Sites of Platelet Activating Factor On the Intact Bovine Cerebral Microvascular Endothelial Cells and Antagonism of Drugs." Zhongguo Yao Li Xue Bao = Acta Pharmacologica Sinica, vol. 13, no. 4, 1992, pp. 326-9.
Sun DX, Rui YC, Zeng GQ, et al. Specific binding sites of platelet activating factor on the intact bovine cerebral microvascular endothelial cells and antagonism of drugs. Zhongguo Yao Li Xue Bao. 1992;13(4):326-9.
Sun, D. X., Rui, Y. C., Zeng, G. Q., Zhu, J., & Shen, Y. A. (1992). Specific binding sites of platelet activating factor on the intact bovine cerebral microvascular endothelial cells and antagonism of drugs. Zhongguo Yao Li Xue Bao = Acta Pharmacologica Sinica, 13(4), 326-9.
Sun DX, et al. Specific Binding Sites of Platelet Activating Factor On the Intact Bovine Cerebral Microvascular Endothelial Cells and Antagonism of Drugs. Zhongguo Yao Li Xue Bao. 1992;13(4):326-9. PubMed PMID: 1333718.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Specific binding sites of platelet activating factor on the intact bovine cerebral microvascular endothelial cells and antagonism of drugs. AU - Sun,D X, AU - Rui,Y C, AU - Zeng,G Q, AU - Zhu,J, AU - Shen,Y A, PY - 1992/7/1/pubmed PY - 1992/7/1/medline PY - 1992/7/1/entrez SP - 326 EP - 9 JF - Zhongguo yao li xue bao = Acta pharmacologica Sinica JO - Zhongguo Yao Li Xue Bao VL - 13 IS - 4 N2 - [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. SN - 0253-9756 UR - https://www.unboundmedicine.com/medline/citation/1333718/Specific_binding_sites_of_platelet_activating_factor_on_the_intact_bovine_cerebral_microvascular_endothelial_cells_and_antagonism_of_drugs_ L2 - http://www.chinaphar.com/1671-4083/13/326.pdf DB - PRIME DP - Unbound Medicine ER -