1265917-14-3
Chemical Structure
S1RA hydrochloride
Synonym(s): E-52862 hydrochloride
- CAS No.: 1265917-14-3
- Formula:C20H24ClN3O2
- Molecular Weight:373.88
IUPAC Name: 4-(2-((5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yl)oxy)ethyl)morpholine hydrochloride
InChIKey: SHRYQZBTQDMGLZ-UHFFFAOYSA-N
SMILES: CC1=CC(OCCN2CCOCC2)=NN1C3=CC(C=CC=C4)=C4C=C3.[H]Cl
Biological Activity: S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a Ki value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (Ki >1000 nM). S1RA hydrochloride is a human 5-HT2B receptor antagonist with an IC50 value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization[1][2].
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S1RA hydrochloride | 99.76% | S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a Ki value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (Ki >1000 nM). S1RA hydrochloride is a human 5-HT2B receptor antagonist with an IC50 value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization. | ||||||||||||||||||||
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- [1]. Romero L, et al. Pharmacological properties of S1RA, a new sigma-1 receptor antagonist that inhibits neuropathic pain and activity-induced spinal sensitization. Br J Pharmacol. 2012 Aug;166(8):2289-306. [Content Brief]
- [2]. Vidal-Torres A, et al. Effects of the selective sigma-1 receptor antagonist S1RA on formalin-induced pain behavior and neurotransmitter release in the spinal cord in rats. J Neurochem. 2014 Jan 3. [Content Brief]
Keywords
