PeptideDB

(S)-Willardiine

CAS: 21416-43-3 F: C7H9N3O4 W: 199.16

(S)-Willardiine is a potent agonist of AMPA/kainate receptors with EC50 of 44.8 uM.IC50 value: 44.8 uM(EC50) Target: AMP
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Bioactivity (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 agonistin 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].
Name (S)-Willardiine
CAS 21416-43-3
Formula C7H9N3O4
Molar Mass 199.16
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Reference [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.