tc-2559

TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist with an EC50 of 0.18 μM. It exhibits selectivity for α4β2 receptors over α2β4, α4β4, and α3β4 receptors, with EC50s ranging from 10 to 30 μM. TC-2559 difumarate also demonstrates antinociceptive effects.

TC-2559 free base is an α4β2 nicotinic acetylcholine receptor (nAChR) agonist with an EC50 of 0.18 μM. It shows weaker agonistic effects on β4 subunit nAChR genotypes (α2β4, α4β4, and α3β4 receptors), with EC50 values ranging from 10-30 μM. In vitro, TC-2559 free base enhances dopamine cell firing in the rat ventral tegmental area (VTA), increasing the excitability and bursting activity of VTA dopaminergic neurons. It also inhibits STAT3 to exert anti-inflammatory effects, alleviates mechanical allodynia in mice, and improves cognitive deficits in rats. TC-2559 free base is utilized in neuropathic pain research.

partial agonist of α4β2 nicotinic acetylcholine receptor