| Name | S1RA hydrochloride |
| Description | S1RA hydrochloride (E-52862 hydrochloride) is an effective and specific sigma-1 receptor(σ1R, Ki: 17 nM) antagonist, and has good selectivity against σ2R (Ki > 1000 nM). |
| 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). |
| 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 50 mg/mL (133.74 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.35 mM), Sonication is recommended.
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| Keywords | σ2 | Sigmareceptor | Sigma Receptor | Sigma receptor | S-1RA hydrochloride | S1RA Hydrochloride | S1RA hydrochloride | S1RA | Inhibitor | inhibit | E-52862 Hydrochloride | E52862 Hydrochloride | E-52862 | E52862 | E 52862 Hydrochloride | E 52862 |
| Inhibitors Related | Alverine citrate | Sevoflurane | Dapoxetine hydrochloride | Cefaclor monohydrate | Clozapine N-Oxide | Mirtazapine | 1,8-Cineole | Venlafaxine hydrochloride | Cloperastine hydrochloride | Trazodone hydrochloride | Mianserin hydrochloride | Cinchonidine |
| Related Compound Libraries | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Immunology/Inflammation Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |
United States
