In the search for new small molecule drugs against neuropathic pain, we identified 2-{[2-(1-benzylpiperidin-4-yl)ethyl]amino}-6-[methyl(prop-2-yn-1-yl)amino]pyridine-3,5-dicarbonitrile (5) as a polyfunctionalized small pyridine with potent dual-target activities against acetylcholinesterase (AChE) (IC50 = 13 nM) and butyrylcholinesterase (BuChE) (IC50 = 3.1 μM), exhibiting high σ1R affinity (Ki(hσ1R) = 1.45 nM) and 290-fold selectivity over the σ2R subtype. The gene discussed is HRH1; the disease is neuropathic pain.