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BD 1047 dihydrobromide
本半岛bd体育手机客户端 不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
BD 1047 dihydrobromide图片
CAS NO: 138356-21-5
包装与价格：
包装 价格(元)
10mg 电议
50mg 电议
500mg 电议
1g 电议

半岛bd体育手机客户端 介绍
BD-1047 (dihydrobromide) 是 sigma-1 受体的选择性功能拮抗剂，在预测精神分裂症疗效的动物模型中显示出抗精神病活性。
Cas No. 138356-21-5
别名 BD-1047盐酸盐
化学名 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
分子式 C13H20Cl2N2.2HBr
分子量 437.04
溶解度 ≥ 43.9 mg/mL in DMSO with gentle warming, ≥ 43.5 mg/mL in Water with gentle warming
储存条件 Store at -20℃
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
半岛bd体育手机客户端 描述

BD 1047 dihydrobromide is an antagonist of σ1 receptor with Ki values of 0.93 and 47 nM for σ-1 receptor and σ-2 receptor, respectively [1].

σ-receptor is a type of opioid receptor. There are two subtypes of σ-receptor: σ-1 and σ-2.σ-1 receptor plays an important role in stimulating dopamine release and modulating the actions of cocaine.

BD 1047 dihydrobromide is a σ-1 receptor antagonist. BD 1047 reduced the dystonia induced by haloperidol and di-o-tolylguanidine (DTG) in a dose-dependent way [1].

In male Wistar rats, BD1047 (20 or 30 mg/kg) reversed response reinstatement induced by the cocaine discriminative stimulus (SD). However, BD1047 had no effect on sweetened condensed milk (SCM) SD-induced responding [2]. In rats with chronic constriction injury (CCI) of the right sciatic nerve, BD1047 significantly relieved CCI-induced mechanical allodynia during the induction. Also, BD1047 significantly increased the expression of σ-1 receptor in the ipsilateral spinal cord dorsal horn and inhibited N-methyl-D-aspartate receptor subunit 1 (NR1) expression and phosphorylation induced by CCI [3].

References:
[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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