BD-1047-dihydrobromide - Sigma Receptor Antagonist - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBD-1047 dihydrobromideCat. No.: HY-16996ACAS No.: 138356-21-5分式: CHBrClN分量: 437.04作靶點(diǎn): Sigma Receptor作通路: GPCR/G Protein; Neuronal Signaling儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 3

2、6 mg/mL (82.37 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.2881 mL 11.4406 mL 22.8812 mL5 mM 0.4576 mL 2.2881 mL 4.5762 mL10 mM 0.2288 mL 1.1441 mL 2.2881 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 BD-1047 氫溴酸鹽種選擇性的 sigma-

3、1 receptor 受體拮抗劑，作于精神分裂癥動(dòng)物模型，具有抗精神病活性 1。IC50 & Target sigma-1 receptor 1體外研究BD-1047 (dihydrobromide) prevents that Cutamesine reduces the cell death rate induced by light exposure in1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEmurine photoreceptor-derived 661w cells 2.BD-1047 (dihydrobromide) at

4、tenuates that Cutamesine reduces the mitochondrial damage and the elevatedlevel of caspase 3/7 activity 2.體內(nèi)研究 BD-1047 (dihydrobromide) (1-10 mg/kg; i.p.) decreases the Apomorphine (APO)-induced climbing behaviorat the dose of 10 mg/kg in mice 1.BD-1047 (dihydrobromide) counteracts the antidepressan

5、t-like effect induced by co-administration ofpramipexole and sertraline (but not pramipexole and fluoxetine) 3.BD-1047 (dihydrobromide) reduces the increasing expression of pNR1, and reverses the Sig-1 R agonistspotentiated NMDA-induced pain behaviour and pNR1 immunoreactivity 4.Animal Model: Male A

6、lbino Swiss mice (50 days old, 2528 g) 1Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kgAdministration: Intraperitoneal injectionResult: Decreased the APO-induced climbing at the dose of 10 mg/kg in mice.REFERENCES1. Skuza G, et al. Effect of BD 1047, a sigma1 receptor antagonist, in the animal models predictive

7、of antipsychotic activity. PharmacolRep. 2006 Sep-Oct;58(5):626-635.2. Shimazawa M, et al. Effect of a sigma-1 receptor agonist, cutamesine dihydrochloride (SA4503), on photoreceptor cell death againstlight-induced damage. Exp Eye Res. 2015 Mar;132:64-72.3. Rogz Z, et al. Mechanism of synergistic action following co-treatment with pramipexole and fluoxetine or sertraline in the forcedswimming test in rats. Pharmacol Rep. 2006 Jul-Aug;58(4):493-500.McePdfHeightCaution: Product has not been fully validated for medical applications.For re