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Tebanicline

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Tebanicline

Tebanicline
Systematic (IUPAC) name
5-([(2R)-Azetidin-2-yl]methoxy)-2-chloropyridine
Identifiers
CAS Registry Number  YesY
ATC code None
PubChem CID:
IUPHAR/BPS
ChemSpider  N
UNII  YesY
ChEMBL  N
Chemical data
Formula C9H11ClN2O
Molecular mass 198.649
 N   

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.[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]

Tebanicline got as far as Phase II trials in humans,[9] but was dropped from further development due to unacceptable incidence of gastrointestinal side effects.[10] However further research in this area is ongoing,[11][12][13][14] 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.[15][16][17][18]

It acts as a partial agonist at neuronal nicotinic acetylcholine receptors, binding to both the α3β4 and the α4β2 subtypes.[19]

References

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  7. ^ Sorbera LA, Revel L, Leeson PA, Castaner J. ABT-594. Drugs Future 2001; 26: 927-934).
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  15. ^ Lloyd GK, Williams M. Neuronal Nicotinic Acetylcholine Receptors as Novel Drug Targets. Journal of Pharmacology and Experimental Therapeutics. 2000; 292:461-467.
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