Sigma-1 receptor antagonist 1

Modify Date: 2024-01-17 15:40:55

Sigma-1 receptor antagonist 1 Structure
Sigma-1 receptor antagonist 1 structure
Common Name Sigma-1 receptor antagonist 1
CAS Number 1639220-19-1 Molecular Weight 380.31
Density N/A Boiling Point N/A
Molecular Formula C19H23Cl2N3O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Sigma-1 receptor antagonist 1


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].

 Names

Name Sigma-1 receptor antagonist 1

 Sigma-1 receptor antagonist 1 Biological Activity

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.

 Chemical & Physical Properties

Molecular Formula C19H23Cl2N3O
Molecular Weight 380.31