Sigma-1 receptor antagonist 5

• UNSPSC Description:

  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 Antigen:

  Histamine Receptor; Sigma Receptor

• Type:

  Reference compound

• Related Pathways:

  GPCR/G Protein;Immunology/Inflammation;Neuronal Signaling

• Applications:

  Neuroscience-Neuromodulation

• Field of Research:

  Neurological Disease

• Assay Protocol:

  https://www.medchemexpress.com/sigma-1-receptor-antagonist-5.html

• Solubility:

  10 mM in DMSO

• Smiles:

  N#CC1=CC=C(C2=CC=C(OCCCN3CCC(C4=CC=NC=C4)CC3)C=C2)C=C1

• Molecular Weight:

  397.51

• References & Citations:

  [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.

• Shipping Conditions:

  Room temperature

• Clinical Information:

  No Development Reported

• CAS Number:

  2952808-33-0