Tebanicline 作为神经元烟碱乙酰胆碱受体的部分激动剂,与 α3β4 和 α4β2 亚型结合。 Tebanicline 是 Abbott 开发的一种有效的合成烟碱(非阿片类)镇痛药。它是作为一种毒性较小的毒镖蛙衍生化合物地巴替丁的类似物而开发的,其作为镇痛剂比吗啡强约 200 倍,但会产生极其危险的毒副作用。与地巴替丁一样,Tebanicline 在动物和人体试验中均显示出对神经性疼痛的有效镇痛活性,但毒性远低于其母体化合物。
产品描述
Tebanicline (ABT-594, Ebanicline) acts as a partial agonist at neuronal nicotinic acetylcholine receptors, binding to both the α3β4 and the α4β2 subtypes. Tebanicline is an effective synthetic nicotinic (non-opioid) analgesic drug developed by Abbott. It was developed as a less toxic analog of the potent poison dart frog-derived compound epibatidine, which is some 200x stronger than morphine as an analgesic but produces extremely dangerous toxic side effects. Like epibatidine, Tebanicline showed potent analgesic activity against neuropathic pain in both animal and human trials, but with far less toxicity than its parent compound.
Cas No.
198283-73-7
分子式
C9H11ClN2O
分子量
198.65
别名
替巴克兰;Ebanicline;ABT-594;Tebanicline
储存和溶解度
DMSO:Soluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years