- Product NameS1RA hydrochloride
- Brief DescriptionInhibitors
- Purification98.00%
- Biological ActivityS1RA Hcl(E-52862 Hcl) is a potent and selective sigma-1 receptor(1R, Ki=17 nM) antagonist, showed good selectivity against 2R (Ki > 1000 nM). IC50 value: 17 nM (Ki) Target: 1R antagonist in vitro: S1RA behaved as a highly selective 1 receptor antagonist. It showed high affinity for human (Ki= 17 nM) and guinea pig (Ki= 23.5 nM) 1 receptors but no significant affinity for the 2 receptors (Ki > 1000 nM for guinea pig and rat 2 receptors). Moderate affinity (Ki= 328 nM) and antagonistic activity, with very low potency (IC50= 4700 nM) was found at the human 5-HT2B receptor. S1RA showed no significant affinity (Ki > 1 μM or % inhibition at 1 μM < 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 mgkg?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 .
- Target NameSigma receptor antagonist
- CAS No. 1265917-14-3
- Calculated MW 373.87
- Formulation C20H24ClN3O2
- Storage 3 years -20˚C powder;2 years -80˚C in solvent;
