CAS No. : 21416-43-3

Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I002646
Molecular Formula:C7H9N3O4
Molecular Weight:199.16
Target:AMPA/kainate receptor agonist
IC50:44.8 uM(EC50) [1]
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Cat No:I002646
Cas No:21416-43-3

(S)-Willardiine is a potent agonist of AMPA/kainate receptors with EC50 of 44.8 uM.
IC50 value: 44.8 uM(EC50) [1]
Target: AMPA/kainate receptor agonist
in vitro: The (S)- but not (R)-isomers of willardiine and 5-bromowillardiine were potent agonists, producing rapidly but incompletely desensitizing responses [1]. At a concentration of 1.8 mM, Ca2+ inhibited the currents induced by 100 microM willardiine by approximately 50% [2].
in vivo: 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 [3].

[1]. Patneau DK, et al. Activation and desensitization of AMPA/kainate receptors by novel derivatives of willardiine. J Neurosci. 1992 Feb;12(2):595-606.
[2]. Fukushima T, et al. Calcium inhibits willardiine-induced responses in kainate receptor GluR6(Q)/KA-2. Neuroreport. 2001 Jan 22;12(1):163-7.
[3]. Gressens P, 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.

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