Sigma-1 receptor antagonist 5 (compound 12),a 4-pyridylpiperidine derivative with analgesic activity,is an antagonist of sigma receptor (Ki=4.5 nM (σ1R),10 nM (σ2R)) and histamine H3 (hH 3 R,Ki=7.7 nM, IC 50 =215 nM). Sigma-1 receptor antagonist 5 suppresses Capsaicin-induced nociception with antinociceptive activity and shows potent efficacy in nociceptive and neuropathic pain models.
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