TC-2559 difumarate

TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC50=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. Antinociceptive effect[1][2].

Signaling Pathways >> Membrane Transporter/Ion Channel >> nAChR

Signaling Pathways >> Neuronal Signaling >> nAChR

Research Areas >> Neurological Disease

TC-2559 difumarate (1-10 mg/kg; i.p.) dose dependently reduces acute formalin-induced biphasic nociceptive responses in mice[2]. TC-2559 difumarate (0.3-3 mg/kg; i.p.) dose dependently inhibits CCI-induced neuropathic pain in rats[2]. Animal Model: Adult male mice (body weight 15-30 g) (formalin test)[2] Dosage: 1, 3, 10 mg/kg Administration: I.p. Result: Dose dependently reduced both early and late phases of formalin induced nociceptive behavioral responses. Animal Model: Adult male SD rats (body weight 200-220 g) (chronic constriction injury (CCI))[2] Dosage: 0.3, 1, 3 mg/kg Administration: I.p. Result: Significantly reversed CCI induced the paw withdrawal threshold decreases.

[1]. Bencherif M, et al. TC-2559: a novel orally active ligand selective at neuronal acetylcholine receptors. Eur J Pharmacol. 2000;409(1):45-55.

[2]. Cheng LZ, et al. Enhanced inhibitory synaptic transmission in the spinal dorsal horn mediates antinociceptive effects of TC-2559. Mol Pain. 2011;7:56. Published 2011 Aug 4.