TC-2559 (free base)

TC-2559 free base is a α4β2 nicotinic acetylcholine receptor (nAChR) agonists with an EC50 of 0.18 μM. TC-2559 free base shows much weaker potencies on the group of b4-containing nAChR subtypes, α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. TC-2559 free base can increase the discharge of dopamine cells in the ventral tegmental area (VTA) of rats in vitro, enhancing the excitability and aggressive behavior of VTA dopamine neurons. TC-2559 free base inhibits STAT3 to exert anti-inflammatory properties and relieves mice mechanical allodynia and improve rats cognitive deficits. TC-2559 free base can be used for the study of nerve pain[1][2][3][4][5].

Product Specifications

CAS Number

[189274-78-0]

UNSPSC

12352005

Target

NAChR; STAT

Related Pathways

JAK/STAT Signaling; Membrane Transporter/Ion Channel; Neuronal Signaling; Stem Cell/Wnt

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Neurological Disease

Smiles

CNCC/C=C/C1=CN=CC(OCC)=C1

Molecular Formula

C12H18N2O

Molecular Weight

206.28

References & Citations

[1]Bencherif M, et al. TC-2559: a novel orally active ligand selective at neuronal acetylcholine receptors. Eur J Pharmacol. 2000 Dec 1;409 (1) :45-55.|[2]Wang Y, et al. TC-2559 excites dopaminergic neurones in the ventral tegmental area by stimulating alpha4beta2-like nicotinic acetylcholine receptors in anaesthetised rats. Br J Pharmacol. 2006 Feb;147 (4) :379-90.|[3]Kiguchi N, et al. TC-2559, an α4β2 nicotinic acetylcholine receptor agonist, suppresses the expression of CCL3 and IL-1β through STAT3 inhibition in cultured murine macrophages. J Pharmacol Sci. 2015 Jun;128 (2) :83-6.|[4]Kiguchi N, et al. Inhibition of peripheral macrophages by nicotinic acetylcholine receptor agonists suppresses spinal microglial activation and neuropathic pain in mice with peripheral nerve injury. J Neuroinflammation. 2018 Mar 27;15 (1) :96.|[5]Chen Y, et al. The nicotinic alpha 4 beta 2 receptor selective agonist, TC-2559, increases dopamine neuronal activity in the ventral tegmental area of rat midbrain slices. Neuropharmacology. 2003 Sep;45 (3) :334-44.