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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]. | [Biological Activity]
TC 2559 difumarate is a subtype-selective partial agonist for α4β2 nicotinic acetylcholine receptors (EC50 values are 0.18, 12.5, 14.0, > 30, > 100 and > 100 μM for α4β2, α4β4, α2β4, α3β4, α3β2 and α7 receptor subtypes respectively). Displays selectivity for (α4)2(β2)3 receptor stoichiometry and enhanced CNS-PNS selectivity ratio. Attenuates scopolamine-induced cognitive deficits in a step-through passive avoidance task. | [in vivo]
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.
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| 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.
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Desiccate at RT | [References]
[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. DOI:10.1016/s0014-2999(00)00807-4
[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. DOI:10.1016/s0028-3908(03)00189-8 |
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