货号 | 5297/50 |
别名 | N-[2-(4'-Cyano[1,1'-biphenyl]-4-yl)pr |
供应商 | Tocris |
生物活性 | Selective 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 vitroandin 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. |
运输条件 | Blue Ice |
存放说明 | 4℃ |
纯度 | >98 % |
计算分子量 | 342.46 |
分子式 | C19H22N2O2 |
可溶性/溶解性 | Soluble to 100 mM in DMSO and to 50 mM in ethanol |
参考文献 | Vosset al (2007) Molecular mechanisms of neurite growth with AMPA receptor potentiation. Neuropharmacology 52 590. PMID: 17101156. O'Neillet 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. Baumbargeret 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. |