Huwentoxin-I (HwTx-I) is a 33-residue peptide toxin that was originally isolated from the venom of the Chinese bird spider Ornithoctonus huwena. Huwentoxin-I is known to be an inhibitor of tetrodotoxin-sensitive voltage-gated Na+ channels (TTX-S) with IC50 values of ~50 nM and N-type voltage-sensitive Ca2+ channels with IC50 values of ~100 nM in mammalian DRG, hippocampus and insect DUM neurons. It has only a very weak effect on L-type Ca2+ channels, no effect on TTX-R channels and has virtually no effect on muscle Na+ channels. The selectivity of Huwentoxin-I for Ca2+ channels appears to be higher than ω-conotoxin MVIIA and equivalent to ω-conotoxin GVIA. Huwentoxin-I demonstrates an antinociceptive effect in the rat model of the formalin test when administrated intrathecally (ED50 ~0.28 µg/kg), without side effects of the ones caused by ω-conotoxin MVIIA.
产品描述
A Blocker of TTX-Sensitive NaV, N-Type Ca2+ Channels and nAChRs
产品形式
Huwentoxin-I (HwTx-I) is a 33-residue peptide toxin that was originally isolated from the venom of the Chinese bird spider Ornithoctonus huwena. Huwentoxin-I is known to be an inhibitor of tetrodotoxin-sensitive voltage-gated Na+ channels (TTX-S) with IC50 values of ~50 nM and N-type voltage-sensitive Ca2+ channels with IC50 values of ~100 nM in mammalian DRG, hippocampus and insect DUM neurons. It has only a very weak effect on L-type Ca2+ channels, no effect on TTX-R channels and has virtually no effect on muscle Na+ channels. The selectivity of Huwentoxin-I for Ca2+ channels appears to be higher than ω-conotoxin MVIIA and equivalent to ω-conotoxin GVIA. Huwentoxin-I demonstrates an antinociceptive effect in the rat model of the formalin test when administrated intrathecally (ED50 ~0.28 µg/kg), without side effects of the ones caused by ω-conotoxin MVIIA.
