170568-47-5
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- CAS号:
- 170568-47-5
- 英文名:
- U-101017
- 英文别名:
- U-101017;PNU 101017;U101017,U 101017;Imidazo[1,5-a]quinoline-3-carboxylic acid, 7-chloro-5-[[(3R,5S)-3,5-dimethyl-1-piperazinyl]carbonyl]-, 1,1-dimethylethyl ester, rel-
- 中文名:
- 170568-47-5
- 中文别名:
- 化合物 T17188
- CBNumber:
- CB43175598
- 分子式:
- C23H27ClN4O3
- 分子量:
- 442.94
- MOL File:
- 170568-47-5.mol
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170568-47-5化学性质
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密度:
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1.33±0.1 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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酸度系数(pKa):
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8.16±0.60(Predicted)
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170568-47-5性质、用途与生产工艺
U-101017 是 benzodiazepine 受体 和 GABAA 受体 的部分激动剂,具有抗焦虑的作用。
PNU-101017 potentiates GABA-stimulated Cl
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currents at low concentrations (<1 μM). U-101017 concentration-dependently inhibits the binding of [
3
H]FNZ to the membrane preparation of rat cerebral cortex in vitro with K
i
of 3.37±0.22 nM.
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 [
3
H]FNZ binding to the mouse cerebral cortex. U-101017 dose-dependently decreases the levels of cGMP with ED
50
s 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.
170568-47-5
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170568-47-5, 170568-47-5 相关搜索:
- 化合物 T17188
- 170568-47-5
- U101017,U 101017
- Imidazo[1,5-a]quinoline-3-carboxylic acid, 7-chloro-5-[[(3R,5S)-3,5-dimethyl-1-piperazinyl]carbonyl]-, 1,1-dimethylethyl ester, rel-
- PNU 101017
- U-101017