| CAS NO: | 138356-21-5 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 437.04 |
| Cas No. | 138356-21-5 |
| Formula | C13H20Cl2N2·2HBr |
| Solubility | insoluble in ETOH; ≥43.5 mg/mL in H2O with gentle warming; ≥43.9 mg/mL in DMSO with gentle warming |
| Chemical Name | N1-(3,4-dichlorophenethyl)-N1,N2,N2-trimethylethane-1,2-diamine dihydrobromide |
| Canonical SMILES | ClC1=CC(CCN(C)CCN(C)C)=CC=C1Cl.Br.Br |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
BD 1047 dihydrobromide是一种σ1受体拮抗剂,作用于σ-1受体和σ-2受体的Ki值分别为0.93和47 nM [1].
σ受体是一类阿片受体.σ受体有两种亚型:σ-1和σ-2.σ-1受体在刺激多巴胺释放和调控可卡因行为中起重要作用.
BD 1047 dihydrobromide是一种σ-1受体拮抗剂. BD 1047剂量依赖性地减少氟哌啶醇和二邻甲苯基胍(DTG)引起的肌张力障碍[1].
在雄性Wistar大鼠中,BD1047(20或30 mg/kg)逆转可卡因辨别性刺激(SD)引起的应答复原.然而,BD1047对甜炼乳(SCM)SD诱导的应答没有影响[2].在右侧坐骨神经慢性压迫性损伤(CCI)大鼠中,BD1047显著减轻CCI诱导的机械性异常疼痛.此外,BD1047显著增加同侧脊髓背角中σ-1受体的表达,并抑制CCI诱导的N-甲基-D-天冬氨酸受体亚基1(NR1)表达和磷酸化[3].
参考文献：
[1]. Matsumoto RR, Bowen WD, Tom MA, et al. Characterization of two novel sigma receptor ligands: antidystonic effects in rats suggest sigma receptor antagonism. Eur J Pharmacol, 1995, 280(3): 301-310.
[2]. Martin-Fardon R, Maurice T, Aujla H, et al. Differential effects of sigma1 receptor blockade on self-administration and conditioned reinstatement motivated by cocaine vs natural reward. Neuropsychopharmacology, 2007, 32(9): 1967-1973.
[3]. Roh DH, Kim HW, Yoon SY, et al. Intrathecal injection of the sigma(1) receptor antagonist BD1047 blocks both mechanical allodynia and increases in spinal NR1 expression during the induction phase of rodent neuropathic pain. Anesthesiology, 2008, 109(5): 879-889.
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