211311-95-4
211311-95-4 結構式
基本信息
N-[2-[4-(4-氰基苯基)苯基]丙基]丙烷-2-磺酰胺
CS-2739
LY404187
LY-404187
LY 404187
N-2-(4-(4-Cyanophenyl)phenyl)propyl-2-propanesulfonamide
N-(2-(4'-cyanobiphenyl-4-yl)propyl)propane-2-sulfonaMide
N-[2-[4-(4-Cyanophenyl)phenyl]propyl]propane-2-sulfonamide
N-[2-(4'-Cyano[1,1'-biphenyl]-4-yl)propyl]-2-propanesulfonamide
N-(2-(4'-Cyano-[1,1'-biphenyl]-4-yl)propyl)propane-2-sulfonaMide
2-Propanesulfonamide, N-[2-(4'-cyano[1,1'-biphenyl]-4-yl)propyl]-
物理化學性質
常見問題列表
EC50: 5.65 μM (GluR1i), 0.15 μM (GluR2i), 1.44 μM (GluR2o), 1.66 μM (GluR3i), 0.21 μM (GluR4i)
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 (EC
50
=1.3±0.3 μM) 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 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. |