LY 404187

Product Description

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.

Solubility

Preparing Stock Solutions for LY 404187

The following data is based on the product molecular weight 342.46

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.92 mL	14.60 mL	29.20 mL
5 mM	0.58 mL	2.92 mL	5.84 mL
10 mM	0.29 mL	1.46 mL	2.92 mL
50 mM	0.06 mL	0.29 mL	0.58 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Baumbarger 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. J.Pharmacol.Exp.Ther. 2001 PMID: 11408529
• Quirk and Nisenbaum LY404187: a novel positive allosteric modulator of AMPA receptors. CNS Drug Rev. 2002 PMID: 12353058
• Voss Molecular mechanisms of neurite growth with AMPA receptor potentiation. Neuropharmacology 2007 PMID: 17101156
• O'Neill Neurotrophic actions of the novel AMPA receptor potentiator, LY404187, in rodent models of Parkinson's disease. Eur.J.Pharmacol. 2004 PMID: 14975705