| Bioactivity | 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]. |
| Invitro | S1RA hydrochloride (0.1-10000 nM) 对人和豚鼠的 σ1R 的 Ki 值分别为 17 和 23.5 nM[1]。 S1RA hydrochloride (0.1-10000 nM) 对人 σ2R 具有亲和力，Ki 值为 9.3 μM[1]。 S1RA hydrochloride 对人 5-HT2B 受体具有亲和力，Ki 值为 328 nM，IC50 值为 4.7 μM[1]。 |
| In Vivo | S1RA hydrochloride (腹腔注射 16-80 mg/kg 或口服 32-128 mg/kg；一次) 剂量依赖性地抑制小鼠中福尔马林诱导的痛觉，辣椒素诱导的机械超敏反应和坐骨神经损伤诱导的机械和热超敏反应[1]。 Animal Model: |
| Name | S1RA hydrochloride |
| CAS | 1265917-14-3 |
| Formula | C20H24ClN3O2 |
| Molar Mass | 373.88 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 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. [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. |
S1RA hydrochloride
CAS: 1265917-14-3 F: C20H24ClN3O2 W: 373.88
S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a Ki value of 17
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