LY 404187

Biological Activity

LY 404187 is a selective AMPA receptor positive allosteric modulator (IC₅₀ values are 0.15, 0.21, 1.66 and 5.65 μM for GluA2_i, GluA4_i, GluA3_i and GluA1_i respectively). Potentiates glutamate and AMPA-evoked currents in prefrontal cortex (PFC) pyramidal neurons in vitro. Has no effect on NMDA- or kainate-evoked currents; also has no effect on K⁺ or Na⁺ ion channels. Potentiates PFC glutamatergic synaptic transmission in vitro and in vivo. Induces neurite growth in combination with (S)-AMPA (Cat. No. 0254) in SH-SY5Y human neuroblastoma cells in vitro. Also reduces MPTP-induced toxicity in mice. Brain penetrant.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Positive modulation of alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptors in prefrontal cortical pyramidal neurons by a novel allosteric potentiator.
   Baumbarger et al.
   J.Pharmacol.Exp.Ther., 2001;298:86
2. Neurotrophic actions of the novel AMPA receptor potentiator, LY404187, in rodent models of Parkinson's disease.
   O'Neill et al.
   Eur.J.Pharmacol., 2004;486:163
3. LY404187: a novel positive allosteric modulator of AMPA receptors.
   Quirk and Nisenbaum
   CNS Drug Rev., 2002;8:255
4. Molecular mechanisms of neurite growth with AMPA receptor potentiation.
   Voss et al.
   Neuropharmacology, 2007;52:590

Product Datasheets