| RRC ID |
62079
|
| 著者 |
Saruhashi S, Konoki K, Yotsu-Yamashita M.
|
| タイトル |
The voltage-gated sodium ion channel inhibitory activities of a new tetrodotoxin analogue, 4,4a-anhydrotetrodotoxin, and three other analogues evaluated by colorimetric cell-based assay.
|
| ジャーナル |
Toxicon
|
| Abstract |
The voltage-gated sodium ion channel inhibitory activities of four tetrodotoxin analogues were evaluated for their ability to reduce the cytotoxicity of ouabain and veratridine in mouse neuroblastoma Neuro-2a cells. EC50 of the novel analogue, 4,4a-anhydrotetrodotoxin purified from pufferfish, was 750 fold larger than that of tetrodotoxin, supporting the implication of 4-OH in activity. The high activity of 11-oxotetrodotoxin was confirmed. Modification of C-6 of 11-nortetrodotoxin-6,6-diol to form an oxime derivative decreased the activity to 1/22.
|
| 巻・号 |
119
|
| ページ |
72-6
|
| 公開日 |
2016-9-1
|
| DOI |
10.1016/j.toxicon.2016.05.012
|
| PII |
S0041-0101(16)30141-6
|
| PMID |
27212630
|
| MeSH |
Animals
Cell Line, Tumor
Ion Channel Gating*
Mice
Sodium Channel Blockers / pharmacology*
Tetrodotoxin / analogs & derivatives*
Tetrodotoxin / toxicity
|
| IF |
2.201
|
| リソース情報 |
| ヒト・動物細胞 |
NB2a(RCB2639) |
