S1RA hydrochloride

• CAT Number: I006566
• CAS Number: 1265917-14-3
• Molecular Formula: C20H24ClN3O2
• Molecular Weight: 373.88
• Purity: ≥95%
• Synonyms: 4-[2-(5-methyl-1-naphthalen-2-ylpyrazol-3-yl)oxyethyl]morpholine;hydrochloride
• InChI: 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
• InChIKey: SHRYQZBTQDMGLZ-UHFFFAOYSA-N
• SMILES: CC1=CC(=NN1C2=CC3=CC=CC=C3C=C2)OCCN4CCOCC4.Cl

S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a Ki value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (Ki >1000 nM). S1RA hydrochloride is a human 5-HT2B receptor antagonist with an IC50 value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization[1][2].
S1RA hydrochloride (0.1-10000 nM) shows high affinity to human and guinea pig σ1Rs with Ki values of 17 and 23.5 nM, respectively[1].
S1RA hydrochloride (0.1-10000 nM) shows affinity to human σ2R with Ki values of 9.3 μM[1].
S1RA hydrochloride shows affinity to human 5-HT2B receptor with a Ki value of 328 nM and an IC50 value of 4.7 μM[1].
S1RA hydrochloride (i.p. 16-80 mg/kg or oral administration 32-128 mg/kg; once) dose-dependently inhibits formalin-induced nociception, capsaicin-induced mechanical hypersensitivity and sciatic nerve injury-induced mechanical and thermal hypersensitivity of mice[1].

Reference

[1]. Romero L, et al. Pharmacological properties of S1RA, a new sigma-1 receptor antagonist that inhibits neuropathic pain and activity-induced spinal sensitization. Br J Pharmacol. 2012 Aug;166(8):2289-306.
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[2]. Vidal-Torres 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 Jan 3.
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