(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].
性状
Solid
IC50 & Target[1][2]
AMPA Receptor Kainate Receptor
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : < 1 mg/mL (ultrasonic) (insoluble or slightly soluble)