| 产品描述: | BZAD01 is a selective NMDA NR1A/2B receptor antagonist. |
| 靶点: |
NMDAR |
| 体内研究: |
Parkinsonism was induced by microinjection of the toxin, 6-hydroxydopamine (6-OHDA) into the medial forebrain bundle (MFB) of 40 Sprague-Dawley rats. Parkinsonism and the efficacy of drugs were assessed using a battery of behavioural tests including balance beam, apomorphine-induced rotation, body axis bias or 'curling', head position bias and disengage sensorimotor latency test. The main effects were that BZAD01 co-administration prevented chronic levodopa-induced potentiation of apomorphine rotation. However levodopa-treated rats were slower than either controls or BZAD-01-treated rats in the locomotor test |
| 参考文献: |
1. Beinat C, et al. Structure-activity relationships of N-substituted 4-(trifluoromethoxy)benzamidines with affinity for GluN2B-containing NMDA receptors. Bioorg Med Chem Lett. 2014 Feb 1;24(3):828-30. 2. Warraich ST, et al. Evaluation of behavioural effects of a selective NMDA NR1A/2B receptor antagonist in the unilateral 6-OHDA lesion rat model. Brain Res Bull. 2009 Feb 16;78(2-3):85-90. 3. Leaver KR, et al. Neuroprotective effects of a selective N-methyl-D-aspartate NR2B receptor antagonist in the 6-hydroxydopamine rat model of Parkinson's disease. Clin Exp Pharmacol Physiol. 2008 Nov;35(11):1388-94. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.76 ml |
13.802 ml |
27.604 ml |
| 5 mM |
0.552 ml |
2.76 ml |
5.521 ml |
| 10 mM |
0.276 ml |
1.38 ml |
2.76 ml |
| 50 mM |
0.055 ml |
0.276 ml |
0.552 ml |
|
| 注意: |
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