6-Benzoylheteratisine (Heteratisan-14-one, 6-(benzoyloxy)-20-ethyl-8-hydroxy-1-methoxy-4-meth) is a Aconitum alkaloid. It can inhibits voltage-gated Na+ channels in rat brain synaptosomes

A concentration-dependent inhibitory effect of 6-benzoylheteratisine on aconitine-induced increases in [Na+]i, [Ca2+]i and the release of glutamate.?The IC50 values were 4.1 microM (Na+), 4.8 microM (Ca2+) and 4.8 microM (glutamate release).?Application of 100 microM 6-benzoylheteratisine after stimulation with 5 microM veratridine also reduced the induced [Na+]i and [Ca2+]i with half-lives of 72.1 and 44.7 s, respectively.?Furthermore, 100 microM 6-benzoylheteratisine reduced the ouabain-induced Na+ influx to the same extent as the Na+ channel inhibitor tetrodotoxin, which points to an inhibition of non-activated Na+ channels by 6-benzoylheteratisine.?Additionally, 100 microM 6-benzoylheteratisine failed to affect the release of glutamate and the increase in [Ca2+]i induced by 30 mM KCl, indicating that voltage-gated Ca2+ channels were not affected by 6-benzoylheteratisine.?The data suggest an inhibitory effect of 6-benzoylheteratisine on voltage-gated Na+ channels as the only target, whereas mechanisms of Na+ and Ca2+ homoeostasis and pathways of glutamate release seem not to be affected by the drug[1].