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Willardiine

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Chemical Structure| 21416-43-3 同义名 : (-)-Willardiine
CAS号 : 21416-43-3
货号 : A412916
分子式 : C7H9N3O4
纯度 : 98%
分子量 : 199.164
MDL号 : MFCD00153879
存储条件:

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 (S) -Willardiine is a potent agonist of AMPA/kainate receptors with EC50 of 44.8 uM. Willardiines produce strikingly different degrees of desensitization: at saturating doses the equilibrium response to the weakly desensitizing agonist (S)-5-iodowillardiine was similar in amplitude to the response to kainate and 10 times larger than the response to the strongly desensitizing agonist (S)-willardiine[3]. In newborn mice (P5, histopathology at P10), local injection of the AMPA receptor agonist S-bromo-willardiine at day 5 after birth induced cortical damage and white matter damage, which was reduced in a dose-dependent manner by the AMPA receptor antagonists[4]. At a concentration of 1.8 mM, Ca2+ inhibited the currents induced by 100 microM willardiine by approximately 50%. Ca2+ inhibition of the willardiine-induced response is concentration dependent[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

5.02mL

1.00mL

0.50mL

25.10mL

5.02mL

2.51mL

50.21mL

10.04mL

5.02mL

参考文献

[1]Gressens P, Spedding M, et al. The effects of AMPA receptor antagonists in models of stroke and neurodegeneration. Eur J Pharmacol. 2005 Sep 5;519(1-2):58-67.

[2]Fukushima T, Marshall J, et al. Calcium inhibits willardiine-induced responses in kainate receptor GluR6(Q)/KA-2. Neuroreport. 2001 Jan 22;12(1):163-7.

[3]Patneau DK, Mayer ML, Jane DE, Watkins JC. Activation and desensitization of AMPA/kainate receptors by novel derivatives of willardiine. J Neurosci. 1992;12(2):595-606

[4]Gressens P, Spedding M, Gigler G, et al. The effects of AMPA receptor antagonists in models of stroke and neurodegeneration. Eur J Pharmacol. 2005;519(1-2):58-67

[5]Fukushima T, Marshall J, Sakata K, Shingai R. Calcium inhibits willardiine-induced responses in kainate receptor GluR6(Q)/KA-2. Neuroreport. 2001;12(1):163-167