Sigma-1 receptor antagonist 1

• CAT Number: I017955
• CAS Number: 1639220-19-1
• Molecular Formula: C19H23Cl2N3O
• Molecular Weight: 380.31
• Purity: ≥95%
• Synonyms: 5-chloro-2-(4-chlorophenyl)-4-methyl-6-(3-piperidin-1-ylpropoxy)pyrimidine
• InChI: InChI=1S/C19H23Cl2N3O/c1-14-17(21)19(25-13-5-12-24-10-3-2-4-11-24)23-18(22-14)15-6-8-16(20)9-7-15/h6-9H,2-5,10-13H2,1H3
• InChIKey: MSFUOAXHQLXDAO-UHFFFAOYSA-N
• SMILES: CC1=C(C(=NC(=N1)C2=CC=C(C=C2)Cl)OCCCN3CCCCC3)Cl

Sigma‑1 receptor antagonist 1 (compound 137) is a potent and selective sigma-1 receptor (σ1R) antagonist, with a high binding affinity to σ1R receptor (Ki = 1.06 nM). Sigma‑1 receptor antagonist 1 exhibits antineuropathic pain activity and acts as a promising agent for the treatment of neuropathic pain[1].
Sigma?1 receptor antagonist 1 exhibits a high binding affinity to σ1R receptor (Ki = 1.06 nM) and good σ-1/2 selectivity (1344-fold)[1].
Sigma?1 receptor antagonist 1 exerts dose-dependent antinociceptive effects in mice formalin model and rats CCI models of neuropathic pain[1].

Reference

[1]. Lan Y, et al. Synthesis and biological evaluation of novel sigma-1 receptor antagonists based on pyrimidine scaffold as agents for treating neuropathic pain. J Med Chem. 2014 Dec 26;57(24):10404-23.
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