S1RA

S1RA is a sigma-1 (sigma1) receptor antagonist (Ki = 17 nM). It is selective for sigma1 receptors over sigma2 receptors (Ki = 9,300 nM), as well as a panel of 170 additional receptors at 1 µM. S1RA reduces capsaicin-induced mechanical allodynia, formalin-induced licking and biting behavior, and partial sciatic nerve ligation-induced thermal hyperalgesia in mice (ED50s = 26.3, 43.7, and 18.8 mg/kg, respectively). It also enhances fentanyl- or loperamide-induced analgesia without affecting gastrointestinal transit in mice.Formal Name: 4-[2-[[5-methyl-1-(2-naphthalenyl)-1H-pyrazol-3-yl]oxy]ethyl]-morpholine. CAS Number: 878141-96-9. Synonyms: E-52862. Molecular Formula: C20H23N3O2. Formula Weight: 337.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 15 mg/ml, DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml, Ethanol: 1 mg/ml. lambdamax: 218, 258 nm. SMILES: CC1=CC(OCCN2CCOCC2)=NN1C3=CC(C=CC=C4)=C4C=C3. InChi Code: InChI=1S/C20H23N3O2/c1-16-14-20(25-13-10-22-8-11-24-12-9-22)21-23(16)19-7-6-17-4-2-3-5-18(17)15-19/h2-7,14-15H,8-13H2,1H3. InChi Key: DGPGXHRHNRYVDH-UHFFFAOYSA-N.