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1639220-19-1

1639220-19-1 structure
1639220-19-1 structure
  • Name: Sigma-1 receptor antagonist 1
  • Chemical Name: Sigma-1 receptor antagonist 1
  • CAS Number: 1639220-19-1
  • Molecular Formula: C19H23Cl2N3O
  • Molecular Weight: 380.31
  • Create Date: 2019-12-08 13:47:19
  • Modify Date: 2025-08-25 17:46:24
  • 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].

Name Sigma-1 receptor antagonist 1
Description 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].
Target

Ki: 1.06 nM (σ1R)[1]

In Vitro 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].
In Vivo Sigma‑1 receptor antagonist 1 exerts dose-dependent antinociceptive effects in mice formalin model and rats CCI models of neuropathic pain[1].
References

[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.

Molecular Formula C19H23Cl2N3O
Molecular Weight 380.31
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