Cat. No. 5297
Chemical Name: N-[2-(4'-Cyano[1,1'-biphenyl]-4-yl)pr
Biological ActivitySelective AMPA receptor positive allosteric modulator (IC50 values are 0.15, 0.21, 1.66 and 5.65 μM for GluA2i, GluA4i, GluA3i and GluA1i respectively). Potentiates glutamate and AMPA-evoked currents in pre frontal 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.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Voss et al (2007) Molecular mechanisms of neurite growth with AMPA receptor potentiation. Neuropharmacology 52 590. PMID: 17101156.
O'Neill et al (2004) Neurotrophic actions of the novel AMPA receptor potentiator, LY404187, in rodent models of Parkinson's disease. Eur.J.Pharmacol. 486 163. PMID: 14975705.
Quirk and Nisenbaum (2002) LY404187: a novel positive allosteric modulator of AMPA receptors. CNS Drug Rev. 8 255. PMID: 12353058.
Baumbarger et al (2001) 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. 298 86. PMID: 11408529.
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