TC 2559 difumarate is a subtype-selective partial agonist for AChR α4β2 (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). It displays selectivity for (α4)2(β2)3 receptor stoichiometry and enhanced CNS-PNS slectivity ratio.
1. Bencherif, M., et al. 2000. Eur. J. Pharmacol. 409 45-55. 2. Chen, Y., et al. 2003. Neuropharmacology. 45: 334-344 3. Zwart, R., et al. 2006. Eur. J. Pharmacol. 539: 10-17.
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