2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. GABAA receptor modulator-9

GABAA receptor modulator-9 是一种针对α1β2γ2 亚型，可透过血脑屏障的正变构 GABAA 调节剂。GABAA receptor modulator-9 对α1β2γ2具有极好的活性 (EC50：在卵母细胞中为 0.9 μM，在 CHO 细胞中为 0.2 μM)，对 α1β2、α3β2γ2 和 α1β3γ2 也有活性 (EC50 分别为 1.3、3.4 和 1.1 μM)。GABAA receptor modulator-9 显著抑制癫痫发作的进展并降低小鼠死亡率。GABAA receptor modulator-9 可用持续性癫痫 (SE) 的研究。

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GABAA receptor modulator-9

GABAA receptor modulator-9 Chemical Structure

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GABAA receptor modulator-9 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-9 is and positive allosteric modulator of a1β2y2 subtype GABAA that can cross the blood-brain barrier. GABAA receptor modulator-9 exhibits comparable activity on α1β2γ2 (EC50: 0.9 μM in oocytes, 0.2 μM in CHO cells) and on α1β2, α3β2γ2 and α1β3γ2 (EC50s of 1.3, 3.4 and 1.1 μM). GABAA receptor modulator-9 significantly suppresses seizure progression and reduces delayed mortality. GABAA receptor modulator-9 can be used for the study of status epilepticus (SE)[1].

体外研究
(In Vitro)

GABAA receptor modulator-9 (Compound (S)-9d) 对 α1 亚基表现出最高的选择性，可能不表现出 β 亚基选择性，而 γ2 亚基不影响其对 GABAARs 的变构活性[1]。

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

GABAA receptor modulator-9 相关抗体:
体内研究
(In Vivo)

GABAA receptor modulator-9 (Compound (S)-9d) (5-30 mg/kg, i.p., 单次给药) 能避免 90% 小鼠出现第 V 阶段的癫痫发作，并且显著延缓了 Pilocarpine (HY-B0726A) 诱导的持续性癫痫和戊四氮诱导的急性惊厥[1]。

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

Animal Model: Pilocarpine-induced status epilepticus (SE) models established in male C57BL/6N mice (6−8 weeks old, 18-20 g)[1]
Dosage: 5, 10 and 30 mg/kg
Administration: Intraperitoneal injection (i.p.), single dose
Result: Exhibited potent therapeutic efficacy, preventing 90% of Stage V seizure onset at 30 mg/kg.
Animal Model: Pentylenetetrazole (PTZ)-induced acute convulsive seizures model established in male C57BL/6N mice (6−8 weeks old, 18-20 g)[1]
Dosage: 5, 10 and 30 mg/kg
Administration: Intraperitoneal injection (i.p.), single dose
Result: Showed reduced seizure suppression compared to diazepam at equivalent doses during the acute 2 h SE phase at 5 mg/kg.
Achieved 90% prevention of Stage V seizures and significantly delayed the latency to Stage III seizure onset at 30 mg/kg.
Induced mild sedative side effects at doses above 20 mg/kg.
分子量

415.53

Formula

C23H17N3OS2
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-9 相关分类

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  • 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:

GABAA receptor modulator-9GABAA receptor modulator9GABAA receptor modulator 9GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorStatus epilepticusoocytesCHO cellsXenograft modelInhibitorinhibitorinhibit

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