化学信息：
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化学名
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4-[2-(5-methyl-1-naphthalen-2-ylpyrazol-3-yl)oxyethyl]morpholine
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简称
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S1RA
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别名
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E-52862, E52862, E 52862
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中文名
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N/A
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化学式
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C20H23N3O2
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分子量
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337.42
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CAS号
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878141-96-9
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纯度
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98%
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溶剂/溶解度
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Water<1mg/ml; DMSO40mg/ml; Ethanol<1mg/ml
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溶液配制
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5mg加入1.48ml DMSO，或者每3.37mg加入1ml DMSO，配制成10mM溶液。SD2393-10mM用DMSO配制。
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生物信息：
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产品描述
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S1RA (E-52862) is a potent and selective sigma-1 receptor (σ1R, Ki=17nM) antagonist, showed good selectivity against σ2R (Ki>1000nM).
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信号通路
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GPCR & G Protein
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靶点
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σ1R
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σ2R
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－
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－
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－
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IC50
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17nM (Ki)
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>1000nM (Ki)
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－
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－
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－
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体外研究
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S1RA behaved as a highly selective σ1 receptor antagonist. It showed high affinity for human (Ki=17nM) and guinea pig (Ki=23.5nM) σ1 receptors but no significant affinity for the σ2 receptors (Ki>1000nM for guinea pig and rat σ2 receptors). Moderate affinity (Ki=328nM) and antagonistic activity, with very low potency (IC50=4700nM) was found at the human 5-HT2B receptor. S1RA showed no significant affinity (Ki>1μM or % inhibition at 1μM <50%) for other additional 170 targets (receptors, transporters, ion channels and enzymes).
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体内研究
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Control (non-operated) and nerve-injured mice received a single or repeated (twice daily for 12 days) i.p. administration of S1RA at 25mg·kg/L, the same dose used for the assessment of behavioural hypersensitivity in the chronic treatment study. Acute treatment was given on day 12 post-surgery and repeated treatment with S1RA started the day of surgery, as in the behavioural studies. Intrathecal pre-treatment with idazoxan prevented the systemic S1RA antinociceptive effect, suggesting that the S1RA antinociception depends on the activation of spinal α2 -adrenoceptors which, in turn, could induce an inhibition of formalin-evoked glutamate release. When administered locally, intrathecal S1RA inhibited only the flinching behavior, whereas intracerebroventricularly or intraplantarly injected also attenuated the lifting/licking behavior.
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临床实验
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N/A
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特征
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N/A
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相关实验数据(此数据来自于公开文献，碧云天并不保证其有效性)：
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酶活性检测实验
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方法
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N/A
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细胞实验
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细胞系
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N/A
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浓度
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N/A
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处理时间
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N/A
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方法
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N/A
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动物实验
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动物模型
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N/A
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配制
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N/A
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剂量
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N/A
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给药方式
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N/A
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参考文献：
1. Díaz JL, et al. J Med Chem. 2012 Oct 11, 55(19), 8211-24.
2. Romero L, et al. Br J Pharmacol. 2012 Aug, 166(8), 2289-306.
包装清单：
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产品编号
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产品名称
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包装
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SD2393-10mM
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S1RA (Sigma Receptor拮抗剂)
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10mM×0.2ml
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SD2393-5mg
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S1RA (Sigma Receptor拮抗剂)
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5mg
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SD2393-25mg
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S1RA (Sigma Receptor拮抗剂)
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25mg
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—
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说明书
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1份
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保存条件：
-20℃保存，至少一年有效。5mg和25mg包装也可室温保存，至少6个月有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。
注意事项：
本产品仅限于专业人员的科学研究用，不得用于临床诊断或治疗，不得用于食品或药品，不得存放于普通住宅内。
为了您的安全和健康，请穿实验服并戴一次性手套操作。
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