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S1RA hydrochloride (E-52862 hydrochloride) 是高活性和选择性的sigma-1受体(σ1R)拮抗剂,Ki为17nM,而对σ2R的Ki则高于1000nM。
产品别名:
4-[2-[[5-甲基-1-(2-萘基)-1H-吡唑-3-基]氧基]乙基]吗啉盐酸盐(1:1)
[1]. Díaz JL, et al. Synthesis and biological evaluation of the 1-arylpyrazole class of σ(1) receptor antagonists: identification of 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862). J Med Chem. 2012 Oct 11;55(19):8211-24.
[2]. 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.
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