(S) -Willardiine

(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].

Product Specifications

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.