S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor ( σ1R ) antagonist with a K i value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (K i >1000 nM). S1RA hydrochloride is a human 5-HT2B receptor antagonist with an IC 50 value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization In Vitro S1RA hydrochloride (0.1-10000 nM) shows high affinity to human and guinea pig σ1Rs with K i values of 17 and 23.5 nM, respectively. S1RA hydrochloride (0.1-10000 nM) shows affinity to human σ2R with K i values of 9.3 μM. S1RA hydrochloride shows affinity to human 5-HT2B receptor with a K i value of 328 nM and an IC 50 value of 4.7 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male CD1 mice 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. Animal Model: Male CD1 mice with formalin-evoked nociception 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. Animal Model: Male CD1 mice with capsaicin-induced mechanical hypersensitivity 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. Form:Solid IC50& Target:Sigma 1 Receptor
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S1RA hydrochloride
Dangerous GoodsCAS number:1265917-14-3 molecular formula:C20H24ClN3O2
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Specs
| Chinese alias | S1RA盐酸盐 | ||
| English alias | A903622 | 4-tert.Butylcalix[4]arene | E-52862 hydrochloride | UNII-18XZ7850YN | E-52862 HCl | S1RA (hydrochloride) | BS177543 | HY-18099A | 18XZ7850YN | 4-(2-(5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy)ethyl)morpholine hydrochloride | SB17182 | BCP24 | ||
| CAS number | 1265917-14-3 | molecular formula | C20H24ClN3O2 |
| molecular weight | 373.9 g/mol | Exact mass | ≥99% |
| PSA | 39.500 Ų | logp | - |
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Safety information
pictogram:
GHS05 , GHS07
Signal word:
Danger
Hazard Statement:
H302: 吞食有害 H318: 造成严重的眼睛损伤
Statement of Preventive Measures:
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P270: 使用本产品时,请勿进食、饮水或吸烟。 P330: 漱口 P264+P265: 处理后彻底洗手[和…]。不要触摸眼睛。 P301+P317: 如果被吞咽:请寻求医疗帮助。 P305+P354+P338: 如果进入眼睛:立即用水冲洗几分钟。取下隐形眼镜(如果有的话),并且操作简单。继续冲洗。 P317: 寻求紧急医疗救助。
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