產品描述: | BD-1047 (dihydrobromide) is a selective functional antagonist of sigma-1 receptor, shows antipsychotic activity in animal models predictive of efficacy in schizophrenia |
靶點: |
sigma-1 receptor;Sigmareceptor |
體外研究: |
BD-1047 (dihydrobromide) prevents that Cutamesine reduces the cell death rate induced by light exposure in murine photoreceptor-derived 661w cells. BD-1047 (dihydrobromide) attenuates that Cutamesine reduces the mitochondrial damage and the elevated level of caspase 3/7 activity. |
體內研究: |
BD-1047 (dihydrobromide) (1-10 mg/kg; i.p.) decreases the Apomorphine (APO)-induced climbing behavior at the dose of 10 mg/kg in mice. BD-1047 (dihydrobromide) counteracts the antidepressant-like effect induced by co-administration of pramipexole and sertraline (but not pramipexole and fluoxetine). BD-1047 (dihydrobromide) reduces the increasing expression of pNR1, and reverses the Sig-1 R agonists potentiated NMDA-induced pain behaviour and pNR1 immunoreactivity. Animal Model: Male Albino Swiss mice (50 days old, 25–28 g) Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg Administration: Intraperitoneal injection Result: Decreased the APO-induced climbing at the dose of 10 mg/kg in mice. |
參考文獻: |
1. Skuza G, et al. Effect of BD 1047, a sigma1 receptor antagonist, in the animal models predictive of antipsychotic activity. Pharmacol Rep. 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 against light-induced damage. Exp Eye Res. 2015 Mar;132:64-72. 3. Rogóz Z, et al. 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. |
溶解性: |
Soluble in DMSO、H2O |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
2.288 ml |
11.441 ml |
22.881 ml |
5 mM |
0.458 ml |
2.288 ml |
4.576 ml |
10 mM |
0.229 ml |
1.144 ml |
2.288 ml |
50 mM |
0.046 ml |
0.229 ml |
0.458 ml |
|
注意: |
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