Premium
Comparative binding and toxicity of saxitoxin and saxitoxinol in mice and in cultured cells
Author(s) -
Naseem Syed M.,
Creasia Donald A.
Publication year - 1997
Publication title -
iubmb life
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.132
H-Index - 113
eISSN - 1521-6551
pISSN - 1521-6543
DOI - 10.1080/15216549700201391
Subject(s) - saxitoxin , receptor , sodium channel , dissociation (chemistry) , toxicity , chemistry , microbiology and biotechnology , biology , biophysics , sodium , biochemistry , toxin , organic chemistry
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°C.