| Identification | Back Directory | [Name]
S1RA (hydrochloride) | [CAS]
1265917-14-3 | [Synonyms]
177303
S1RA. HCL
S1RA (E-52862) HCI
S1RA HCl (E-52862)
E52862 hydrochloride
S1RA (hydrochloride)
E 52862 hydrochloride
E-52862 hydrochloride
E-52862 HYDROCHLORIDE;E52862 HYDROCHLORIDE;E 52862 HYDROCHLORIDE
4-(2-(5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy)ethyl)morpholine hydrochloride
4-[2-[[5-Methyl-1-(2-naphthalenyl)-1H-pyrazol-3-yl]oxy]ethyl]morpholine hydrochloride (1:1) | [EINECS(EC#)]
931-042-6 | [Molecular Formula]
C20H24ClN3O2 | [MDL Number]
MFCD27963345 | [MOL File]
1265917-14-3.mol | [Molecular Weight]
373.88 |
| Chemical Properties | Back Directory | [storage temp. ]
-20°C (des.) | [solubility ]
Soluble in DMSO (up to at least 25 mg/ml) | [form ]
solid | [color ]
Off-white | [Stability:]
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| Hazard Information | Back Directory | [Description]
S1RA (E-52862, 1265917-14-3) is a potent and selective σ1 antagonist with weak binding at σ2?(IC50?σ1 = 17nM, σ2 = 9300nM).1,2?S1RA abolished mechanical and thermal hyperalgesia in mice with carrageenan-induced acute inflammation by enhancing the action of endogenous opioid peptides of immune origin in a σ1 dependent manner.3?S1RA potentiated μ-opioid antinociception in mice in a σ-dependent manner.4?S1RA displayed neuroprotective effects in a mouse model of ischemic stroke.5 | [Uses]
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]. | [in vivo]
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]. | Animal Model: | Male CD1 mice[1] | | Dosage: | 32, 64, 128 and 160 mg/kg | | Administration: | Intraperitoneal injection; 32, 64, 128 and 160 mg/kg, once | | Result: | Reduced the permanence time on the rotating rod in rotarod test.
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| Animal Model: | Male CD1 mice with formalin-evoked nociception[1] | | Dosage: | 20, 40 and 80 mg/kg | | Administration: |
Intraperitoneal injection; 20, 40 and 80 mg/kg, once | | Result: | Dose-dependently showed analgesic effect on of formalin-evoked nociceptive behaviours of mice.
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| Animal Model: | Male CD1 mice with capsaicin-induced mechanical hypersensitivity[1] | | Dosage: | 16, 32 and 64 mg/kg (i.p.); 32, 64 and 128 mg/kg (oral administration) | | Administration: | Intraperitoneal injection or oral administration; 16, 32 and 64 mg/kg (i.p.); 32, 64 and 128 mg/kg (oral administration), once | | Result: | Dose-dependently reversed capsaicin-induced mechanical hypersensitivity in mice.
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| [IC 50]
Sigma 1 Receptor | [References]
References/Citations |
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| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
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