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S1RA acts as an antagonist at σ1 receptors, exhibiting analgesic and antinociceptive properties. S1RA reverses mechanical and thermal pain sensitivity in animal models of inflammatory pain. In models of neuropathic pain, this compound decreases formalin-induced glutamate release and increases levels of norepinephrine.
| Cas No. | 878141-96-9 |
|---|---|
| Purity | ≥99% |
| Formula | C20H23N3O2 |
| Formula Wt. | 337.42 |
| IUPAC Name | 4-(2-{[5-Methyl-1-(2-naphthyl)-1H-pyrazol-3-yl]oxy}ethyl)morpholine |
| Synonym | E52862, 4-Morpholine |
| Solubility | 10 mM in DMSO |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet |
Gris G, Merlos M, Vela JM, et al. S1RA, a selective sigma-1 receptor antagonist, inhibits inflammatory pain in the carrageenan and complete Freund's adjuvant models in mice. Behav Pharmacol. 2014 Jun;25(3):226-35. PMID: 24776490.
Vidal-Torres A, Fernández-Pastor B, Carceller 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 May;129(3):484-94. PMID: 24384038.
Bura AS, Guegan T, Zamanillo D, et al. Operant self-administration of a sigma ligand improves nociceptive and emotional manifestations of neuropathic pain. Eur J Pain. 2013 Jul;17(6):832-43. PMID: 23172791.