2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. U-101017

U-101017  (Synonyms: PNU 101017)

目录号: HY-19250
产品使用指南

摩尔计算器

U-101017 是 benzodiazepine 受体 和 GABAA 受体 的部分激动剂，具有抗焦虑的作用。

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U-101017 Chemical Structure

U-101017 Chemical Structure

CAS No. : 170568-47-5

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U-101017 相关抗体

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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

U-101017 is a partial agonist of benzodiazepine receptor and GABAA receptor, with anxiolytic effects. 

体外研究
(In Vitro)

PNU-101017 potentiates GABA-stimulated Cl- currents at low concentrations (<1 μM)[1]. U-101017 concentration-dependently inhibits the binding of [3H]FNZ to the membrane preparation of rat cerebral cortex in vitro with Ki of 3.37±0.22 nM[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

U-101017 相关抗体:
体内研究
(In Vivo)

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[1]. 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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

442.94

Formula

C23H27ClN4O3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献
Animal Administration
[1]

Three groups of gerbils (N=9-11/group) are treated i.p. with either vehicle (0.05 N HCl), PNU-101017 (30 mg/kg) or diazepam (10 mg/kg) 30 min prior to ischemia and again 2 h after reperfusion. Two other groups receive PNU-101017 or diazepam immediately after reperfusion and again 2 h later. The tested doses of PNU-101017 and diazepam are selected from past studies demonstrating their neuroprotective efficacy in the gerbil forebrain ischemia model. The administration of the second dose at 2 h after reperfusion is consistent with previous dosing with other effective compounds tested in the gerbil. The 0.05 N HCl vehicle has been employed for i.p. dosing with other test compounds and is devoid of toxicity or acute distress production.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

U-101017 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

U-101017170568-47-5PNU 101017U101017U 101017PNU101017PNU-101017GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorInhibitorinhibitorinhibit

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产品名称：
U-101017
目录号：
HY-19250
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