Overview
- Jane, D.E. et al. (1997) J. Med. Chem. 40, 3645.
- Patneau, D.K. et al. (1992) J. Neurosci. 12, 595.
Alomone Labs (S)-(-)-5-Fluorowillardiine activates AMPA receptors expressed in Xenopus oocytes.Representative time course of GluA1 channel current activation by a continuous application of 50 nM and 500 nM (S)-(-)-5-Fluorowillardiine (#F-205), duration indicated by bars (bottom left), compared to activation by 5 µM (S)-AMPA (#A-267), at a holding potential of -80 mV.
- Jane, D.E. et al. (1997) J. Med. Chem. 40, 3645.
- Patneau, D.K. et al. (1992) J. Neurosci. 12, 595.
- Chizh, B.A. et al. (1994) Br. J. Pharmacol. 112, 843.
- Perrais, D. et al. (2009) Neuropharmacology 56, 131.
(S)-(-)-5-Fluorowillardiine is a highly potent and selective AMPA receptor agonist. 5-Fluorowillardiine is synthesized as two distinct isomers: R and S. (S)-(-)-5-Fluorowillardiine is selective over kainate receptors and is more potent and selective than AMPA itself; at equilibrium, (S)-(-)-5-Fluorowillardiine is seven times more potent than AMPA and 30 times more potent than willardiine. (S)-(-)-5-Fluorowillardiine demonstrates an EC50 value of 1.5 µm1,2.
The ionotropic glutamate AMPA receptors (AMPARs) are the primary receptors mediating fast excitatory synaptic transmission in the mammalian brain. This function is essential for synaptic plasticity and learning and memory3,4.
(S)-(-)-5-Fluorowillardiine (#F-205) is a highly pure, synthetic, and biologically active compound.
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