Baden D G
Rosenstiel School of Marine and Atmospheric Science, University of Miami, Florida 33149.
FASEB J. 1989 May;3(7):1807-17. doi: 10.1096/fasebj.3.7.2565840.
Brevetoxins are lipid-soluble polyether marine toxins of unique structure and pharmacological function. Toxins are active in vivo in the nanomolar to picomolar concentration range and in vitro in isolated neuromuscular or giant axon preparations and in single-cell or subcellular model systems. Their effect is excitatory, mediated by the enhancement of cellular Na+ influx. Brevetoxins bind at site 5 on the voltage-sensitive sodium channel, a specificity shared with ciguatoxin. This site is allosterically linked to other natural toxin binding sites on the channel.
短裸甲藻毒素是具有独特结构和药理功能的脂溶性聚醚类海洋毒素。这些毒素在体内的纳摩尔至皮摩尔浓度范围内具有活性，在体外对分离的神经肌肉或巨大轴突制剂以及单细胞或亚细胞模型系统也有活性。它们的作用是兴奋性的，由细胞内钠离子内流增强介导。短裸甲藻毒素与电压敏感性钠通道的位点5结合，这一特异性与雪卡毒素相同。该位点与通道上的其他天然毒素结合位点存在变构联系。
