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Tebanicline : ウィキペディア英語版
Tebanicline

Tebanicline (Ebanicline, ABT-594) is a potent synthetic nicotinic (non-opioid) analgesic drug developed by Abbott. It was developed as a less toxic analogue 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.〔Sorbera LA, Revel L, Leeson PA, Castaner J. ABT-594. ''Drugs Future'' 2001; 26: 927-934).〕
Tebanicline got as far as Phase II trials in humans, but was dropped from further development due to unacceptable incidence of gastrointestinal side effects. However further research in this area is ongoing, and it is expected that development of new neural nicotinic acetylcholine receptor agonists will be likely to lead to novel analgesics suitable for use in humans within the next few years.〔Lloyd GK, Williams M. Neuronal Nicotinic Acetylcholine Receptors as Novel Drug Targets. ''Journal of Pharmacology and Experimental Therapeutics''. 2000; 292:461-467.〕
It acts as a partial agonist at neuronal nicotinic acetylcholine receptors, binding to both the α3β4 and the α4β2 subtypes.
== References ==




抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
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