| Identification | Back Directory | [Name]
Sigma-1 receptor antagonist 1 | [CAS]
1639220-19-1 | [Synonyms]
Sigma-1 receptor antagonist 1
Pyrimidine, 5-chloro-2-(4-chlorophenyl)-4-methyl-6-[3-(1-piperidinyl)propoxy]-
inhibit,Inhibitor,Sigma-1 receptor antagonist 1,Sigma Receptor,Sigma 1 receptor antagonist 1,Sigma1 receptor antagonist 1 | [Molecular Formula]
C19H23Cl2N3O | [MDL Number]
MFCD32215325 | [MOL File]
1639220-19-1.mol | [Molecular Weight]
380.31 |
| Chemical Properties | Back Directory | [Boiling point ]
439.3±45.0 °C(Predicted) | [density ]
1.219±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 6.25 mg/mL (16.43 mM) | [form ]
Solid | [pka]
8.95±0.10(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
Sigma?1 receptor antagonist 1 exerts dose-dependent antinociceptive effects in mice formalin model and rats CCI models of neuropathic pain[1].
| [IC 50]
Sigma 1 Receptor | [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. DOI:10.1021/jm501207r |
|
|