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 μM。LY-404187 有潜力用于许多精神疾病和神经退行性疾病的研究。
| 生物活性 | LY-404187 is a potent, selective and centrally active positive allosteric modulator ofAMPA receptors, with theEC50s of 5.65, 0.15, 1.44, 1.66 and 0.21 μM forGluR1i,GluR2i,GluR2o,GluR3iandGluR4i, respectively. LY-404187 has therapeutic potential in a number of psychiatric disorders and neurodegenerative diseases[1][2]. |
| IC50& Target | EC50: 5.65 μM (GluR1i), 0.15 μM (GluR2i), 1.44 μM (GluR2o), 1.66 μM (GluR3i), 0.21 μM (GluR4i)[2] |
体外研究
(In Vitro) | LY-404187 (3-10 nM) potentiates glutamate-evoked inward currents in human GluR4 transfected HEK293 cells[2].
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)[3].
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[3].
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体内研究
(In Vivo) | LY-404187 (0.5 mg/kg; s.c for 11 days) can prevent MPTP-induced neurotoxicity in mice[4].
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[4].
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[4].
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[4].
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[4].
| Animal Model: | Male C57BL/6J mice (20-25 g) are challenged with MPTP on day 8[4] | | 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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(292.00 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.9200 mL | 14.6002 mL | 29.2005 mL | | 5 mM | 0.5840 mL | 2.9200 mL | 5.8401 mL | | 10 mM | 0.2920 mL | 1.4600 mL | 2.9200 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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