Naseem S M, Creasia D A
U.S.Army Medical Research Institute of Infectious Diseases, Fort Detrick, Frederick, MD-21702-5011, USA.
Biochem Mol Biol Int. 1997 Feb;41(2):377-88. doi: 10.1080/15216549700201391.
The binding characteristics of saxitoxin (STX), a known voltage-gated sodium channel blocker, and its analog saxitoxinol (STXOL), were studied in neuroblastoma, peritoneal macrophage, hepatocytes and PC-12 cell lines. 3H-STXOL bound to the cell-surface sites which appear to be the same as those occupied by 3H-STX and which can, therefore, be identified as STX receptors. The relative agreement of respective Kd obtained by saturation, competition, association and dissociation kinetics for STX and STXOL suggest the absence of any artifact in binding measurements. Unlike STX, STXOL was non-toxic to mice by intratracheal instillation. The major advantage of using 3H-STXOL is that the tritium label is not exchangeable. Data from this study suggest that 3H-STXOL can be used to identify STX receptors at 37 degrees C.
已知的电压门控钠通道阻滞剂石房蛤毒素（STX）及其类似物石房蛤毒素醇（STXOL）的结合特性，在神经母细胞瘤、腹膜巨噬细胞、肝细胞和PC-12细胞系中进行了研究。3H-STXOL与细胞表面位点结合，这些位点似乎与3H-STX占据的位点相同，因此可被鉴定为STX受体。通过饱和、竞争、结合和解离动力学获得的STX和STXOL各自Kd的相对一致性表明结合测量中不存在任何假象。与STX不同，STXOL经气管内滴注对小鼠无毒。使用3H-STXOL的主要优点是氚标记不可交换。这项研究的数据表明，3H-STXOL可用于在37摄氏度下识别STX受体。
