(S) -Willardiine

• 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].

• CAS Number :

  [21416-43-3]

• Product Name Alternative :

  (-) -Willardiine

• UNSPSC :

  12352005

• Hazard Statement :

  H302, H312, H332

• Target :

  IGluR

• Type :

  Reference compound

• Related Pathways :

  Membrane Transporter/Ion Channel; Neuronal Signaling

• Applications :

  Neuroscience-Neuromodulation

• Field of Research :

  Neurological Disease

• Assay Protocol :

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

• Purity :

  98.93

• Solubility :

  H2O : < 0.1 mg/mL (ultrasonic; warming; heat to 60°C)

• Smiles :

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

• Molecular Formula :

  C7H9N3O4

• Molecular Weight :

  199.17

• Precautions :

  H302, H312, H332

• 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)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  AMPA Receptor; Kainate Receptor