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蝙蝠葛碱和粉防己碱对[3H]WEB 2086与体外牛脑前动脉平滑肌细胞结合的影响(英文)
引用本文:曾国钱,鞠佃文,孙笃新,黄彤舸,芮耀诚.蝙蝠葛碱和粉防己碱对[3H]WEB 2086与体外牛脑前动脉平滑肌细胞结合的影响(英文)[J].药学学报,1993,28(7):499-503.
作者姓名:曾国钱  鞠佃文  孙笃新  黄彤舸  芮耀诚
作者单位:第二军医大学药学院药理教研室,上海200433
摘    要:用标记的血小板活化因子拮抗剂3H]WEB 2086,在培养的牛脑前动脉平滑肌细胞上鉴定了血小板活化因子受体。结果表明在25℃时该细胞上存在两种与配基具有不同亲和力的受体结合位点,其中Kd-1=22.8±5.0 nmol·L-1,Kd-2=186+20.5 nmol·L-1;Bmax-1=2.1±0.3 pmol/104细胞,Bmax-2=12.1±1-5 pmol/106细胞。蝙蝠葛碱和粉防己碱均能抑制3H]WEB2086与上述细胞的结合。

关 键 词:[3H]WEB  2086  血管平滑肌  受体  血小板活化因子  蝙蝠葛碱  粉防己碱
收稿时间:1992-10-19

EFFECTS OF DAURICINE AND TETRANDRINE ON [3H] WEB 2086 SPECIFIC BINDING TO BOVINE ANTERIOR CEREBRAL ARTERIAL SMOOTH MUSCLE CELLS IN VITRO
GQ Zeng,DW Ju,DX Sun,TG Huang and YC Rui.EFFECTS OF DAURICINE AND TETRANDRINE ON [3H] WEB 2086 SPECIFIC BINDING TO BOVINE ANTERIOR CEREBRAL ARTERIAL SMOOTH MUSCLE CELLS IN VITRO[J].Acta Pharmaceutica Sinica,1993,28(7):499-503.
Authors:GQ Zeng  DW Ju  DX Sun  TG Huang and YC Rui
Abstract: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/106 cells and Bmax-2=12.1±1.5 pmol/106cells. 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.
Keywords:Vascular smooth muscle  Receptor  PAF  Dauricine  Tetrandrine  [3H] WEB 2086
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