GAT2711 is a novel full agonist of the alpha9 nicotinic acetylcholine receptor (EC50 = 230 nM, EC50 for alpha9alpha10 = 990 nM). It was 340-fold selective over the alpha7 receptor. GAT2711 significantly and dose-dependently inhibited the BzATP-induced release of the pro-inflammatory cytokine IL-1ß in THP-1 cells (IC50 = 0.5 µM). It fully attenuated inflammatory pain in mice in an alpha7 nAChR-independent manner. alpha9 nAChR agonists represent a novel approach to treating inflammatory and/or neuropathic pain.
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