SML3970
S1RA
≥98% (HPLC)
别名:
4-{2-[5-Methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine, E 52862, E-52862, E52862, MR 309, MR-309, MR309
生化/生理作用
Selective, high-affinity sigma-1 receptor antagonist with antinociceptive efficacy in vivo.
S1RA (E-52862) is a selective, high-affinity sigma-1 receptor antagonist (human/guinea pig σ1 Ki = 17/23.5 nM; σ2 Ki = 9.3 μM/rat, >1 μM/guinea pig). S1RA exerts dose-dependent antinociceptive effects in several neuropathic pain models in mice in vivo (16 - 64 mg/kg i.p.).
S1RA (E-52862) is a selective, high-affinity sigma-1 receptor antagonist (human/guinea pig σ1 Ki = 17/23.5 nM; σ2 Ki = 9.3 μM/rat, >1 μM/guinea pig). S1RA exerts dose-dependent antinociceptive effects in several neuropathic pain models in mice in vivo (16 - 64 mg/kg i.p.).
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
此项目有
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
L Romero et al.
British journal of pharmacology, 166(8), 2289-2306 (2012-03-13)
The sigma-1 (σ(1) ) receptor is a ligand-regulated molecular chaperone that has been involved in pain, but there is limited understanding of the actions associated with its pharmacological modulation. Indeed, the selectivity and pharmacological properties of σ(1) receptor ligands used
José Luis Díaz et al.
Journal of medicinal chemistry, 55(19), 8211-8224 (2012-07-13)
The synthesis and pharmacological activity of a new series of 1-arylpyrazoles as potent σ(1) receptor (σ(1)R) antagonists are reported. The new compounds were evaluated in vitro in human σ(1)R and guinea pig σ(2) receptor (σ(2)R) binding assays. The nature of
Francisco Rafael Nieto et al.
The journal of pain, 13(11), 1107-1121 (2012-10-16)
Sigma-1 (σ(1)) receptors play a role in different types of pain and in central sensitization mechanisms; however, it is unknown whether they are involved in chemotherapy-induced neuropathic pain. We compared the ability of paclitaxel to induce cold (acetone test) and
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