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Tetrapentylammonium block of chloramine‐T and veratridine modified rat brain type IIA sodium channels
Author(s) -
Ghatpande A S,
Rao S,
Sikdar S K
Publication year - 2001
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1038/sj.bjp.0703973
Subject(s) - veratridine , sodium channel , chloramine t , chemistry , block (permutation group theory) , sodium , pharmacology , neuroscience , medicine , biology , mathematics , organic chemistry , geometry
Tetrapentylammonium (TPeA) block of rat brain type IIA sodium channel α subunit was studied using whole cell patch clamp. Results indicate that TPeA blocks the inactivating brain sodium channel in a potential and use‐dependent manner similar to that of the cardiac sodium channel. Removal of inactivation using chloramine‐T (CT) unmasks a time‐dependent block by TPeA consistent with slow blocking kinetics. On the other hand, no time dependence is observed when inactivation is abolished by modification with veratridine. TPeA does not bind in a potential‐dependent fashion to veratridine‐modified channels and does not significantly affect gating of veratridine‐modified channels suggesting that high affinity binding of TPeA to the brain sodium channel is lost after veratridine modification. British Journal of Pharmacology (2001) 132 , 1755–1760; doi: 10.1038/sj.bjp.0703973