Sigma-1 receptor antagonist 5

CAS: F: C26H27N3O W: 397.51

Sigma-1 receptor antagonist 5 (compound 12)，a 4-pyridylpiperidine derivative with analgesic activity，is an antagonist

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Bioactivity	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 (hH3R，Ki=7.7 nM，IC50=215 nM). Sigma-1 receptor antagonist 5 suppresses Capsaicin-induced nociception with antinociceptive activity and shows potent efficacy in nociceptive and neuropathic pain models[1].
Target	Ki: 7.7 nM (σ1R), 4.5 Nm (σ2R), 10 nM (hH3R)
Name	Sigma-1 receptor antagonist 5
Formula	C26H27N3O
Molar Mass	397.51
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Szczepańska K, et al. Dual Piperidine-Based Histamine H3 and Sigma-1 Receptor Ligands in the Treatment of Nociceptive and Neuropathic Pain. J Med Chem. 2023 Jul 27;66(14):9658-9683.