1639220-19-1

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: 2024-01-17 15:40:55
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