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Tebanicline
Chemical compound From Wikipedia, the free encyclopedia
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Tebanicline (ebanicline, ABT-594) is a potent 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 about 200 times stronger than morphine as an analgesic, but produces extremely dangerous toxic side effects.[1][2] 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.[3][4][5][6][7][8] It acts as a partial agonist at neuronal nicotinic acetylcholine receptors, binding to both the α3β4 and the α4β2 subtypes.[9]
Tebanicline progressed to Phase II clinical trials in humans,[10] but was dropped from further development due to unacceptable incidence of gastrointestinal side effects.[11] However, further research in this area is ongoing,[12][13][14][15] and the development of nicotinic acetylcholine receptor agonists is ongoing.[16][17][18][19] No agents from this class have successfully completed human clinical trials due to their unacceptable side effect profiles.
CNS Rev:[20]
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See also
- Ropanicant (SUVN-911)
- Goldstein reported a series of agents that a based on a cyclopropane ring.[21][22][23][24] The following examples are representative: PC10176364 [387844-92-0], PC15980432 & PC16662145. One of these structures could be S-38232. S-35836-1 is another compound that was described in the literature by Goldstein based on the familiar cyclopropyl design.
References
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