Tebanicline
Template:Short descriptionTemplate:Drugbox
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]
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.
References
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- ↑ Solo Goldstein, et al. U.S. patent 6943184 (2002 to ADIR SARL, Laboratoires Servier SAS).
- ↑ Charton Y, Guillonneau C, Lockhart B, Lestage P, Goldstein S. Preparation and affinity profile of novel nico-tinic ligands. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2188-93. doi: 10.1016/j.bmcl.2007.12.075. Epub 2008 Jan 26. PMID: 18262785.
- ↑ US7348344 idem Solo Goldstein, et al. WO2007012762 (Laboratoires Servier SAS).
- ↑ Solo Goldstein, et al. WO2007085750 (to Laboratoires Servier SAS).
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