产品
编 号：F271063
分子式：C19H22N2O2S
分子量：342.46
分子式：C19H22N2O2S
分子量：342.46
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
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5mg
询价
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10mg
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25mg
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询价
结构图
CAS No: 211311-95-4
产品详情
生物活性：
LY-404187 is a potent, selective and centrally active positive allosteric modulator of AMPA receptors, with the EC50s of 5.65, 0.15, 1.44, 1.66 and 0.21 μM for GluR1i, GluR2i, GluR2o, GluR3i and GluR4i, respectively. LY-404187 has therapeutic potential in a number of psychiatric disorders and neurodegenerative diseases.
体内研究：
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.
体外研究：
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 is a potent, selective and centrally active positive allosteric modulator of AMPA receptors, with the EC50s of 5.65, 0.15, 1.44, 1.66 and 0.21 μM for GluR1i, GluR2i, GluR2o, GluR3i and GluR4i, respectively. LY-404187 has therapeutic potential in a number of psychiatric disorders and neurodegenerative diseases.
体内研究：
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.
体外研究：
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.
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