货号:A777046
同义名:
BD-1047 dihydrobromide; BD 1047 (hydrobromide)
BD-1047 2HBr是一种选择性的 sigma 受体功能拮抗剂,在动物模型中表现出抗精神病活性,具有预测精神分裂症疗效的潜力。
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| Type | HazMat fee for 500 gram (Estimated) |
| Excepted Quantity | USD 0.00 |
| Limited Quantity | USD 15-60 |
| Inaccessible (Haz class 6.1), Domestic | USD 80+ |
| Inaccessible (Haz class 6.1), International | USD 150+ |
| Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
| Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |


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|---|---|---|---|---|---|---|---|
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| 描述 | BD-1047 Dihydrobromide is a selective functional antagonist of sigma-1 receptor, shows antipsychotic activity in animal models predictive of efficacy in schizophrenia. BD 1047 did not decrease amphetamine-induced hyperactivity in mice in a statistically significant manner. Likewise, it did not modify the hyperactivity induced by NMDA receptor antagonists, phencyclidine, memantine or dizocilpine. On the other hand, BD 1047 (1-10 mg/kg; i.p.) attenuated apomorphine-induced climbing in mice and phencyclidine-induced head twitches in rats, like rimcazole and panamesine did[3]. BD-1047 Dihydrobromide prevents that Cutamesine reduces the cell death rate induced by light exposure in murine photoreceptor-derived 661w cells. BD-1047 attenuates that Cutamesine reduces the mitochondrial damage and the elevated level of caspase 3/7 activity[4]. Intrathecal (i.t.) pretreatment with the selective sigma-1 receptor antagonist, BD-1047 dihydrobromide (10-100 nmol) dose dependently reduced formalin-induced pain behaviors in second phase, but not first phase, of the formalin test. I.t. injection of BD-1047 also reduced formalin-evoked Fos expression and pNR1 at the protein kinase C-dependent site, serine-896 (Ser896) and the protein kinase A-dependent site, serine-897 (Ser897) in spinal dorsal horn.i.t[5]. |
| Concentration | Treated Time | Description | References | |
| HT22 cells | 1 μM | 1 hour | To verify the antioxidative effect of YL-0919 via σ-1R | Neural Regen Res. 2025 Aug 1;20(8):2325-2336. |
| Administration | Dosage | Frequency | Description | References | ||
| ICR mice | Formalin-induced pain model | Intrathecal injection | 10–100 nmol | Single administration, observed for 30 minutes | BD-1047 dose-dependently reduced formalin-induced pain behaviors in the second phase but not the first phase. Additionally, BD-1047 reduced formalin-evoked Fos expression and pNR1 (Ser896 and Ser897) expression in the spinal dorsal horn. | Br J Pharmacol. 2006 Jun;148(4):490-8 |
| ICR mice | Chronic constriction injury (CCI) model | Intrathecal injection | 100 nmol | Twice daily on post-operative days 0–3 | BD-1047 significantly attenuated CCI-induced mechanical allodynia (MA) but not thermal hyperalgesia (TH). BD-1047 also reduced CCI-induced astrocyte activation and p38 MAPK phosphorylation. | Br J Pharmacol. 2014 Dec;171(24):5881-97 |
| Guinea pigs | Citric-acid-induced cough model | Intraperitoneal injection | 1–5mg/kg | Single dose, 30 minutes pretreatment | BD-1047 reversed the inhibition of cough elicited by SKF-10,047, indicating its role as a sigma-1 receptor antagonist | Br J Pharmacol. 2004 Jan;141(2):233-40 |
| Rats | KA-induced seizure model | Intraperitoneal injection | 1 or 2 mg/kg | Single administration, 15 minutes before pretreatment | BD-1047 significantly counteracted the anticonvulsant effects of dextromethorphan or dimemorfan on KA-induced seizure behaviors, suggesting that its action is partly related to σ1 receptor activation. | Br J Pharmacol. 2005 Apr;144(7):908-18 |
| C57BL/6J mice | Traumatic brain injury model | Intragastric gavage | 4 mg/kg | Once daily for 3 days | To verify the neuroprotective effect of YL-0919 via σ-1R | Neural Regen Res. 2025 Aug 1;20(8):2325-2336. |
| Mice | Mechanical allodynia model | Intrathecal injection | 10, 30, 100 nmol | Single injection | BD-1047 significantly reduced DHEAS-induced mechanical allodynia, indicating that sigma-1 receptors play an important role in DHEAS-induced allodynia. | Br J Pharmacol. 2009 Jun;157(4):666-73 |
| ICR mice | NMDA-induced pain model | Intrathecal injection | 100 nmol | Single dose, observed for 60 minutes | BD-1047 significantly reduced the increased pNR1 expression induced by Sig-1R agonists PRE-084 or carbetapentane and reversed NMDA-induced pain behaviors | Br J Pharmacol. 2008 Jul;154(5):1125-34 |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.29mL 0.46mL 0.23mL |
11.44mL 2.29mL 1.14mL |
22.88mL 4.58mL 2.29mL |
|
| CAS号 | 138356-21-5 |
| 分子式 | C13H22Br2Cl2N2 |
| 分子量 | 437.04 |
| SMILES Code | CN(C)CCN(CCC1=CC=C(Cl)C(Cl)=C1)C.[H]Br.[H]Br |
| MDL No. | MFCD00792739 |
| 别名 | BD-1047 dihydrobromide; BD 1047 (hydrobromide); BD-1047 HBr |
| 运输 | 蓝冰 |
| InChI Key | WOALTFHGLDVJHK-UHFFFAOYSA-N |
| Pubchem ID | 45073418 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, 2-8°C |
| 溶解方案 |
DMSO: 25 mg/mL(57.2 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO H2O: 25 mg/mL(57.2 mM),配合低频超声助溶 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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