(S)-Willardiine

• Product Name Alternative:

  (-)-Willardiine

• UNSPSC Description:

  (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].

• Target Antigen:

  iGluR

• Type:

  Reference compound

• Related Pathways:

  Membrane Transporter/Ion Channel;Neuronal Signaling

• Field of Research:

  Neurological Disease

• Assay Protocol:

  https://www.medchemexpress.com/_S_-Willardiine.html

• Purity:

  99.27

• Smiles:

  N[C@@H](CN(C(N1)=O)C=CC1=O)C(O)=O

• Molecular Weight:

  199.166

• References & Citations:

  [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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Clinical Information:

  No Development Reported

• CAS Number:

  21416-43-3