Compound 2-(3,4-dichlorophenoxy)-N-(2-morpholin-4-ylethyl)acetamide (1) was designed, prepared and the in vitro binding evaluation against σ₁ and σ₂ receptors was measured. Compound 1 showed high σ₁ receptor affinity (K_i=42nM) and it was 36-times more selective for σ₁ than σ₂ receptor. Also, it was performed a molecular docking of compound 1 into the ligand binding pocket homology model of σ₁ receptor, showing a salt bridge between the ionized morpholine ring and Asp126, as well as important short contacts with residues Tyr120, His154 and Trp164. Ligand efficiency indexes and predicted toxicity analysis revealed an excellent intrinsic quality of 1. The antinociceptive effect of compound 1 was determined using the formalin test. The ipsilateral local peripheral (10–300μg/paw) and intrathecal (100μg/rat) administration of 1 produced a reduction in formalin-induced nociception. The in vivo results indicated that 1 may be effective in treating inflammatory pain.