A σ1 receptor antagonist
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Alternative(s)
16279S1RA
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S1RA (hydrochloride)

Item No. 32729

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[2-[[5-methyl-1-(2-naphthalenyl)-1H-pyrazol-3-yl]oxy]ethyl]-morpholine, monohydrochloride
CAS Number
1265917-14-3
Synonyms
  • E-52862
  • P 027
Molecular Formula
C20H23N3O2 • HCl
Formula Weight
373.9
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMF:PBS (pH 7.2) (1:5): 0.16 mg/mlDMSO: 1 mg/ml
λmax
217, 258 nm
SMILES
CC1=CC(OCCN2CCOCC2)=NN1C3=CC(C=CC=C4)=C4C=C3.Cl
InChi Code
InChI=1S/C20H23N3O2.ClH/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;1H
InChi Key
SHRYQZBTQDMGLZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    25 mg

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    Product Description

    S1RA is a sigma-1 (σ1) receptor antagonist (Ki = 17 nM).1 It is selective for σ1 receptors over σ2 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.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Romero, L., Zamanillo, D., Nadal, X., et al. Pharmacological properties of S1RA, a new sigma-1 receptor antagonist that inhibits neuropathic pain and activity-induced spinal sensitization. Br. J. Pharmacol. 166(8), 2289-2306 (2012).

    2. Sánchez-Fernández, C., Montilla-García, Á., González-Cano, R., et al. Modulation of peripheral μ-opioid analgesia by σ1 receptors. J. Pharmacol. Exp. Ther. 348(1), 32-45 (2014).