2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. GABAA receptor modulator-13

GABAA receptor modulator-13 是一种口服有效的具有血脑屏障穿透性的 α4β1δ GABAA 受体调节剂 (IC50 = 9.02 μM)。GABAA receptor modulator-13 可降低 GABA 诱导的电流，破坏 α4β1δ GABAA 受体跨膜结构域 M2-M3 环的稳定性，且对含 γ2 的 GABAA 受体亚型及 α6β3δ GABAA 受体亚型具有选择性。GABAA receptor modulator-13 可用于神经发育障碍和癫痫等紧张性抑制改变的神经系统疾病的研究。

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GABAA receptor modulator-13

GABAA receptor modulator-13 Chemical Structure

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GABAA receptor modulator-13 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-13 is an orally active, blood-brain barrier-permeable α4β1δ GABAA receptor modulator (IC50 = 9.02 μM). GABAA receptor modulator-13 reduces GABA-induced currents, impairs the stability of the transmembrane domain M2-M3 loop of α4β1δ GABAA receptors, and exhibits selectivity for γ2-containing GABAA receptor subtypes and α6β3δ GABAA receptor subtypes. GABAA receptor modulator-13 is applicable to the research of nervous system diseases with altered tonic inhibition, such as neurodevelopmental disorders and epilepsy[1].

体外研究
(In Vitro)

GABAA receptor modulator-13 (Compound 1e) (0.1-100 μM; 10 s preapplication, followed by 5 s coapplication with 1 μM GABA) 是人源重组 α4β1δ GABAₐ 受体的负性变构调节剂，其 IC50 为 9.02 μM[1]。
GABAA receptor modulator-13 (1-30 μM; 10 s preapplication, followed by 5 s coapplication with 1 μM GABA) 可浓度依赖性地抑制人重组 α4(T300I)β1δ 和 α4β1δ(L260V) 功能获得型 GABAA受体的 GABA 诱导电流[1]。
GABAA receptor modulator-13 (10 μM; 5 s coapplication with 1 μM GABA) 可显著加快人重组 α4β1δ GABAA 受体上 GABA 诱导电流的衰减[1]。

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

GABAA receptor modulator-13 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 (Elimination)
Mice[1] 10 mg/kg p.o. 1.25 h
体内研究
(In Vivo)

GABAA receptor modulator-13 (10 mg/kg; p.o.; single dose) 在雄性 CD-1 小鼠中单次灌胃给予 10 mg/kg 剂量后显示出可检测的脑穿透性，其在 Cmax 时的脑-血浆比值为 0.26，且该剂量下耐受性良好[1]。

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

Animal Model: CD-1 (male)[1]
Dosage: 10 mg/kg
Administration: p.o.; single dose
Result: Reached a brain concentration of 97 ng/g and plasma concentration of 3742 ng/mL at 0.5 hours (Cmax).
Resulted in a brain-plasma ratio of 0.26 and an unbound partition coefficient (Kp,uu) of 0.22.
Exhibited a plasma half-life of 1.25 hours.
Showed no gross abnormalities or signs of discomfort in mice.
分子量

364.83

Formula

C20H17ClN4O
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-13 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

GABAA receptor modulator-13GABAA receptor modulator13GABAA receptor modulator 13GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid Receptorα4β1δ GABAA receptor modulatorneurodevelopmental disordersepilepsyCD-1 mice
Inhibitorinhibitorinhibit

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