蝙蝠葛碱和粉防己碱对<sup>3</sup>HWEB 2086与体外牛脑前动脉平滑肌细胞结合的影响(英文)

蝙蝠葛碱和粉防己碱对³HWEB 2086与体外牛脑前动脉平滑肌细胞结合的影响(英文)

摘要: 用标记的血小板活化因子拮抗剂³HWEB 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K_d-1=22.8±5.0 nmol·L^-1,K_d-2=186+20.5 nmol·L^-1;B_max-1=2.1±0.3 pmol/10⁴细胞,B_max-2=12.1±1-5 pmol/10⁶细胞。蝙蝠葛碱和粉防己碱均能抑制³HWEB2086与上述细胞的结合。

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 K_d-1=22.8±5.0 nmol.L^-1, K_d-2=186±20.5 nmol.L^-1 at 25 C. The total number of binding sites were B_max-1=2.1±0.3 pmol/10⁶ cells and B_max-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.