产品
编 号：F204574
分子式：C23H27ClN4O3
分子量：442.94
分子式：C23H27ClN4O3
分子量：442.94
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CAS No: 170568-47-5
产品详情
生物活性：
U-101017 is a partial agonist of benzodiazepine receptor and GABAA receptor, with anxiolytic effects.
体内研究：
Pre-ischemic treatment with either PNU-101017 significantly protects the CA1 neuronal population, and PNU-101017 reduces the loss to 50%. Delaying PNU-101017 administration until immediately after reperfusion does not reduce the neuroprotective activity. U-101017 (30 μmol/kg, p.o.) time-dependently blocks [3H]FNZ binding to the mouse cerebral cortex. U-101017 dose-dependently decreases the levels of cGMP with ED50s of 260.0 (163-425) and 0.37 (0.12-1.04) in nonstressed and foot shock-stressed mice, respectively. Flumazenil, an antagonist of GABAA receptors, has no significant effect on cGMP in nonstressed mice, but pretreatment with flumazenil significantly blocks U-101017 (10 μmol/kg, p.o.)-induced reductions in cGMP. In stressed mice, flumazenil is ineffective in altering cerebellar cGMP, but pretreatment with these doses of flumazenil significantly (p < 0.01) blocks U-101017-induced attenuation of stress-induced elevations in cGMP.
体外研究：
PNU-101017 potentiates GABA-stimulated Cl- currents at low concentrations (U-101017 相关抗体:
U-101017 is a partial agonist of benzodiazepine receptor and GABAA receptor, with anxiolytic effects.
体内研究：
Pre-ischemic treatment with either PNU-101017 significantly protects the CA1 neuronal population, and PNU-101017 reduces the loss to 50%. Delaying PNU-101017 administration until immediately after reperfusion does not reduce the neuroprotective activity. U-101017 (30 μmol/kg, p.o.) time-dependently blocks [3H]FNZ binding to the mouse cerebral cortex. U-101017 dose-dependently decreases the levels of cGMP with ED50s of 260.0 (163-425) and 0.37 (0.12-1.04) in nonstressed and foot shock-stressed mice, respectively. Flumazenil, an antagonist of GABAA receptors, has no significant effect on cGMP in nonstressed mice, but pretreatment with flumazenil significantly blocks U-101017 (10 μmol/kg, p.o.)-induced reductions in cGMP. In stressed mice, flumazenil is ineffective in altering cerebellar cGMP, but pretreatment with these doses of flumazenil significantly (p < 0.01) blocks U-101017-induced attenuation of stress-induced elevations in cGMP.
体外研究：
PNU-101017 potentiates GABA-stimulated Cl- currents at low concentrations (U-101017 相关抗体:
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