Zeng G Q, Ju D W, Sun D X, Huang T G, Rui Y C
Department of Pharmacology, School of Pharmacy, Second Military Medical University, Shanghai.
Yao Xue Xue Bao. 1993;28(7):499-503.
By using [3H] WEB 2086, a PAF antagonist, specific binding sites of PAF on bovine anterior cerebral arterial smooth muscle cells was identified. Two populations of binding sites with different dissociation constants on the cells were found. The Kd-1 = 22.8 +/- 5.0 nmol.L-1, Kd-2 = 186 +/- 20.5 nmol.L-1 at 25 C. The total number of binding sites were Bmax-1 = 2.1 +/- 0.3 pmol/10(6) cells and Bmax-2 = 12.1 +/- 1.5 pmol/10(6) cells. Dauricine and tetrandrine, two active compounds with similar chemical structure extracted from traditional Chinese herbs, were found to inhibit [3H] WEB 2086 specific binding significantly in culture cells.
通过使用血小板活化因子(PAF)拮抗剂[3H] WEB 2086,确定了PAF在牛大脑前动脉平滑肌细胞上的特异性结合位点。在这些细胞上发现了两类具有不同解离常数的结合位点。在25℃时,Kd-1 = 22.8 +/- 5.0 nmol.L-1,Kd-2 = 186 +/- 20.5 nmol.L-1。结合位点的总数分别为Bmax-1 = 2.1 +/- 0.3 pmol/10(6)个细胞和Bmax-2 = 12.1 +/- 1.5 pmol/10(6)个细胞。从传统中药中提取的两种化学结构相似的活性化合物蝙蝠葛碱和粉防己碱,在培养细胞中能显著抑制[3H] WEB 2086的特异性结合。