LY404187

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

LY404187 是 AMPA 受体的正变构调节剂。

LY404187 is a positive allosteric modulator of AMPA receptors.

LY-404187 (3-10 nM) potentiates glutamate-evoked inward currents in human GluR4 transfected HEK293 cells.LY-404187 (0.03-10 μM) selectively enhances glutamate-evoked currents through AMPA receptor/channels of acutely isolated pyramidal neurons with considerably greater potency (EC50=1.3±0.3 μM) and efficacy (Emax=45.3±8.0-fold increase) .LY-404187 does not affect the magnitude or time course of wholecell K+ or Na+ currents in pre frontal cortex (PFC) pyramidal neurons at concentrations of 10 μM.

LY-404187 (0.5 mg/kg; s.c for 11 days) can prevent MPTP-induced neurotoxicity in mice.LY-404187 (0.5 mg/kg; s.c. for 28 days) attenuates apomorphine-induced contraversive rotations and affords significant protection against the loss of tyrosine hydroxylase positive nigral cell bodies.LY-404187 (0.1 or 0.5 mg/kg; s.c. for 14 days) affords functional, neurochemical and histological protection after infusion of 6-hydroxydopamine into the substantia nigra in rats.LY-404187 (0.5 mg/kg; s.c. for 14 days) delayed treatment provides functional and histological improvement, suggesting a trophic action as administration is initiated after cell death.LY-404187 (0.1 and 0.5 mg/kg; s.c. for 14 days) increases GAP-43 immunoreactivity in the striatum in a dose-dependent manner. Animal Model:Male C57BL/6J mice (20-25 g) are challenged with MPTP on day 8 Dosage:0.5 mg/kg Administration:S.c; twice daily on weekdays and once daily at weekends for 11 days Result:Attenuated the loss of tyrosine hydroxylase immunoreactivity in the substantia nigra.No significant change in tyrosine hydroxylase immunoreactivity in the dorsal and ventral striatum.

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Neuroscience

GluR

AMPA

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211311-95-4

342.46

C19H22N2O2S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (292.00 mM)

CC(CNS(=O)(=O)C(C)C)c1ccc(-c2ccc(C#N)cc2)cc1

2-Propanesulfonamide N-(2-(4'-cyano(11'-biphenyl)-4-yl)propyl)-

(-20℃)

With Ice Pack

≥ 2 years