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LY-404187

CAS No. : 211311-95-4

MCE 站：LY-404187

产品活性：LY-404187 是有效的，选择性和中枢活性的 AMPA 受体的正变构调节剂，作用于 GluR1i，GluR2i，GluR2o，GluR3i 和 GluR4i 的 EC₅₀ 值分别为 5.65、0.15、1.44、1.66 和 0.21 ?M。LY-404187 有潜力用于许多精神疾病和神经退行性疾病的研究。

研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：iGluR

In Vitro: LY-404187 (3-10 nM) potentiates glutamate-evoked inward currents in human GluR4 transfected HEK293 cells.
LY-404187 (0.03-10 ?M) selectively enhances glutamate-evoked currents through AMPA receptor/channels of acutely isolated pyramidal neurons with considerably greater potency (EC₅₀=1.3±0.3 ?M) and efficacy (E_max=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 ?M.

In Vivo: 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.

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