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)  

EFFECTS OF DAURICINE AND TETRANDRINE ON [~3H] WEB 2086 SPECIFIC BINDING TO BOVINE ANTERIOR CEREBRAL ARTERIAL SMOOTH MUSCLE CELLS IN VITRO

作　　者：曾国钱[1] 鞠佃文[1] 孙笃新[1] 黄彤舸[1] 芮耀诚[1] 

机构地区：[1]第二军医大学药学院药理教研室,上海200433

出　　处：《药学学报》1993年第7期499-503,共5页Acta Pharmaceutica Sinica

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/10~4细胞,B_(max-2)=12.1±1-5 pmol/10~6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。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/10~6 cells and B_(max-2)=12.1±1.5 pmol/10~6cells. 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.

关 键 词：血管平滑肌 蝙蝠葛碱 粉防己碱 

分 类 号：R963[医药卫生—微生物与生化药学]