2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. GABAA receptor modulator-10

GABAA receptor modulator-10 是一种具有口服活性、强效的 α1β2γ2 GABAA receptor 正变构调节剂 (PAM)，具有良好的血脑屏障渗透性。GABAA receptor modulator-10 增强 α1β2γ2 GABAA receptor 功能并增强 GABA 诱发的电流。GABAA receptor modulator-10 在 Pentetrazol (PTZ) 和 Kainic Acid (KA) (HY-N2309) 诱导的小鼠癫痫模型中显示出强大的抗癫痫功效。GABAA receptor modulator-10 可用于癫痫研究。

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GABAA receptor modulator-10

GABAA receptor modulator-10 Chemical Structure

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GABAA receptor modulator-10 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GABAA receptor modulator-10 is an orally active, potent positive allosteric modulator (PAM) of the α1β2γ2 GABAA receptor with favorable blood-brain barrier (BBB) penetration. GABAA receptor modulator-10 enhances α1β2γ2 GABAA receptor function and potentiates GABA-evoked currents. GABAA receptor modulator-10 demonstrates potent antiepileptic efficacy in both the Pentetrazol (PTZ)- and Kainic Acid (KA) (HY-N2309)-induced mice epilepsy models. GABAA receptor modulator-10 can be used for the study of epilepsy[1].

IC50 & Target[1]

α1β2γ2 GABAA receptor

 

体外研究
(In Vitro)

GABAA receptor modulator-10 (Compound 10) (10 μM) 通过基于 MQAE 的荧光测定法，增强过表达 α1β2γ2 GABAA receptor 的 HEK293T 细胞中 α1β2γ2 GABAA receptor 的功能[1]。
GABAA receptor modulator-10 (0.1-100 μM) 通过膜片钳测定法，以浓度依赖性方式增强过表达 α1β2γ2 GABAA receptor 的 HEK293T 细胞中 GABA 诱发的电流 (EC50 = 1.99 μM，Emax = 80.1%)[1]。

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

GABAA receptor modulator-10 相关抗体:
体内研究
(In Vivo)

GABAA receptor modulator-10 (Compound 10) (10 μM，在 PTZ 处理前暴露 3 小时) 减少了 6 天后受精的 AB 型斑马鱼的总移动距离[1]。
GABAA receptor modulator-10 (0.3-30 mg/kg，口服，在 PTZ 注射前 1 小时) 延长了 PTZ 诱导的小鼠癫痫模型中 I 期癫痫和 III 期癫痫的潜伏期，缩短了 III 期癫痫的持续时间，并防止了 V 期癫痫的发生[1]。
GABAA receptor modulator-10 (30 mg/kg，口服，在 KA 注射前 30 分钟) 减轻了 KA 诱导的小鼠颞叶癫痫模型中的癫痫严重程度，并降低了死亡率[1]。

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

Animal Model: PTZ-induced mouse epilepsy model: Male KM mice (18-20 g) were were subcutaneously injected with 85 mg/kg PTZ (dissolved in saline) to induce seizures[1]
Dosage: 0.3 mg/kg, 1 mg/kg, 10 mg/kg, 30 mg/kg
Administration: p.o., 1 h before PTZ injection
Result: Prolonged the latency of stage I seizures by 1.21-, 0.96-, 1.53-, and 2.20-fold, and stage III seizures by 1.02-, 1.03-, 1.22-, and 1.45-fold, respectively.
Shortened the duration of stage III seizures.
Animal Model: KA-induced mouse temporal lobe epilepsy (TLE) model: Male C57B6/J mice (18-20 g) were intraperitoneally injected with 30 mg/kg kainic acid (KA, dissolved in saline) to induce TLE[1]
Dosage: 30 mg/kg
Administration: p.o., 30 min before KA injection
Result: Attenuated seizure severity.
Showed comparable effect to diazepam.
分子量

395.82

Formula

C20H15ClFN5O
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

GABAA receptor modulator-10 相关分类

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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:

GABAA receptor modulator-10GABAA receptor modulator10GABAA receptor modulator 10GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid Receptorepilepsyα1β2γ2 GABAA receptorInhibitorinhibitorinhibit

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