tebanicline-tosylate

Description: Tebanicline tosylate (also known as ABT-594 tosylate, Ebanicline tosylate and ABT594 tosylate) is a novel, potent, orally bioavailable nAChR modulator with effective analgesic activity. It inhibits the binding of cytisine to alpha4beta2 neuronal nAChRs with a Ki of 37 pM. Tebanicline is a potent synthetic nicotinic (non-opioid) analgesic drug developed by Abbott 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. It acts as a partial agonist at neuronal nicotinic acetylcholine receptors, binding to both the alpha3beta4 and the alpha4beta2 subtypes.

References: J Physiol Paris. 1998 Jun-Aug; 92(3-4):221-4.; Eur J Pharmacol. 1998 Apr 3; 346(1):23-33.

Related CAS: 203564-54-9 (HCl); 198283-73-7 (free base); 209326-19-2 (2HCl); 209326-18-1 (benzoate)