S1RA

SKU: orb1303040

Description

S1RA hydrochloride (E-52862 hydrochloride) is a potent and selective sigma-1 receptor (σ1R) antagonist with a Ki of 17 nM, demonstrating over 1000-fold selectivity versus the σ2R. This tool compound is widely used in preclinical research to investigate σ1R function in models of neuropathic pain, neurodegenerative diseases, and psychiatric disorders.

Research Area

Neuroscience

Key Properties

• CAS Number: 1265917-14-3
• MW: 373.88
• Purity: >98%
• Formula: C₂₀H₂₃N₃O₂·HCl
• SMILES: Cl.Cc1cc(OCCN2CCOCC2)nn1-c1ccc2ccccc2c1
• Target: ER/Golgi
• Solubility: Soluble in DMSO (up to at least 25 mg/ml)

Bioactivity

• Target IC50:
  σ1 receptor:17 nM
• In Vivo:
  Control (non-operated) and nerve-injured mice received a single or repeated (b.i.d, for 12 days) S1RA (25 mg/kg, i.p.), the same dose used for the assessment of behavioral hypersensitivity in the chronic treatment study. In the behavioral studies, acute treatment was given on day 12 post-surgery and repeated treatment with S1RA started the day of surgery. Intrathecal pre-treatment with idazoxan prevented the systemic S1RA antinociceptive effect, suggesting that the S1RA antinociception depends on the activation of spinal α2 -adrenoceptors which, in turn, could induce an inhibition of formalin-evoked glutamate release. When administered locally, intrathecal S1RA inhibited only the flinching behavior, whereas intracerebroventricularly or intraplantarly injected also attenuated the lifting/licking behavior.
• In Vitro:
  S1RA showed high affinity for the guinea pig (Ki: 23.5 nM) and human (Ki: 17 nM) σ1 receptors but no marked affinity for the σ2 receptors (Ki > 1000 nM for guinea pig and rat σ2 receptors). Moderate affinity (Ki: 328 nM) and antagonistic activity with very low potency (IC50: 4700 nM) were found at the human 5-HT2B receptor. S1RA showed a low affinity (Ki > 1 μM, IC50>1 μM) for other additional 170 targets (transporters, receptors, ion channels and enzymes).

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

E-52862 HCl

Compound Identifiers

PubChem CID

50914801