Sigma-1 receptor antagonist 3

Names

[ CAS No. ]:
1639220-17-9

[ Name ]:
Sigma-1 receptor antagonist 3

Biological Activity

[Description]:

Sigma-1 receptor antagonist 3 (compound135) is a potent and selective Sigma-1 (σ1) receptor antagonist with a Ki of 1.14 nM. Sigma-1 receptor antagonist 3 inhibits Human Ether-a-go-go-Related Gene (hERG) with an IC50 of 1.54 μM. Sigma-1 receptor antagonist 3 is for treating neuropathic pain[1].

[Target]

IC50: 1.54μM (hERG)[1]. Ki : 1.14 nM (Sigma-1 receptor); 1239 nM (Sigma-2 receptor) [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 ]:
C19H23ClFN3O

[ Molecular Weight ]:
363.86

Related Compounds