Kukel C F, Jennings K R
Agricultural Research Division, American Cyanamid Co., Princeton, NJ 08540.
Can J Physiol Pharmacol. 1994 Jan;72(1):104-7. doi: 10.1139/y94-016.
A series of C19-diterpenoid alkaloids purified from Delphinium were evaluated as inhibitors of alpha-bungarotoxin binding to rat and house fly neural membranes. In comparing these diterpenoid analogs, a wide range of inhibition potencies (IC50) were observed, with calculated IC50 values ranging six orders of magnitude. The most potent inhibitory alkaloids in this series possessed the succinimide aromatic ester moiety in the C18 position. Glaudelsine had an IC50 value of 42 pM at the insect nicotinic acetylcholine receptor.
从翠雀属植物中纯化得到的一系列C19-二萜生物碱被评估为α-银环蛇毒素与大鼠和家蝇神经膜结合的抑制剂。在比较这些二萜类似物时，观察到了广泛的抑制效力（IC50），计算得到的IC50值范围跨越六个数量级。该系列中最有效的抑制性生物碱在C18位具有琥珀酰亚胺芳香酯部分。格劳德辛在昆虫烟碱型乙酰胆碱受体处的IC50值为42 pM。
