产品说明书

BD-1047 2HBr

Print
Chemical Structure| 138356-21-5 同义名 : BD-1047 dihydrobromide;BD 1047 (hydrobromide);BD-1047 HBr
CAS号 : 138356-21-5
货号 : A777046
分子式 : C13H22Br2Cl2N2
纯度 : 98%
分子量 : 437.041
MDL号 : MFCD00792739
存储条件:

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

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

动物实验配方:
生物活性
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].
实验方案
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

参考文献

[1]Skuza G, Rogoz Z. Effect of BD 1047, a sigma1 receptor antagonist, in the animal models predictive of antipsychotic activity. Pharmacol Rep. 2006 Sep-Oct;58(5):626-35.

[2]Rogoz Z, Skuza G. Mechanism of synergistic action following co-treatment with pramipexole and fluoxetine or sertraline in the forced swimming test in rats. Pharmacol Rep. 2006 Jul-Aug;58(4):493-500.

[3]Skuza G, Rogóz Z. Effect of BD 1047, a sigma1 receptor antagonist, in the animal models predictive of antipsychotic activity. Pharmacol Rep. 2006 Sep-Oct;58(5):626-35

[4]Shimazawa M, Sugitani S, Inoue Y, Tsuruma K, Hara H. Effect of a sigma-1 receptor agonist, cutamesine dihydrochloride (SA4503), on photoreceptor cell death against light-induced damage. Exp Eye Res. 2015 Mar;132:64-72

[5]Kim HW, Kwon YB, Roh DH, Yoon SY, Han HJ, Kim KW, Beitz AJ, Lee JH. Intrathecal treatment with sigma1 receptor antagonists reduces formalin-induced phosphorylation of NMDA receptor subunit 1 and the second phase of formalin test in mice. Br J Pharmacol. 2006 Jun;148(4):490-8