Sigma-1 receptor antagonist 1
Names
[ CAS No. ]:
1639220-19-1
[ Name ]:
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]
Chemical & Physical Properties
[ Molecular Formula ]:
C19H23Cl2N3O
[ Molecular Weight ]:
380.31