S1RA hydrochloride
Cat. No. :YN321174
CAS No. :1265917-14-3
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order@ubiochem.com| Product Name: | S1RA hydrochloride |
| CAS NO.: | 1265917-14-3 |
| Chemical Name: | |
| Synonyms: | |
| Molecular Weight: | 373.88 |
| Molecular Formula: | C₂₀H₂₄ClN₃O₂ |
| SMILES: | CC1=CC(OCCN2CCOCC2)=NN1C3=CC(C=CC=C4)=C4C=C3.[H]Cl |
| Storage: | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Transportation: | Room temperature in continental US; may vary elsewhere. |
| Description: | S1RA hydrochloride (E-52862 hydrochloride) is a potent and selective sigma-1 receptor(σ1R, Ki=17nM) antagonist, showed good selectivity against σ2R (Ki > 1000nM).in vitro: S1RA behaved as a highly selective σ1 receptor antagonist. It showed high affinity for human (Ki= 17nM) and guinea pig (Ki= 23.5nM) σ1 receptors but no significant affinity for the σ2 receptors (Ki > 1000nM for guinea pig and rat σ2 receptors). Moderate affinity (Ki= 328nM) and antagonistic activity, with very low potency (IC50= 4700nM) was found at the human 5-HT2B receptor. S1RA showed no significant affinity (Ki > 1μM or % inhibition at 1μM < 50%) for other additional 170 targets (receptors, transporters, ion channels and enzymes) . in vivo: Control (non-operated) and nerve-injured mice received a single or repeated (twice daily for 12 days) i.p. administration of S1RA at 25 mg·kg 1, the same dose used for the assessment of behavioural hypersensitivity in the chronic treatment study. Acute treatment was given on day 12 post-surgery and repeated treatment with S1RA started the day of surgery, as in the behavioural studies . 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 . |
| IC50&Target: | |
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