1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. iGluR
  3. AMPA receptor modulator-9

AMPA 受体调节剂-9 是一种具有血脑屏障通透性、口服活性的、选择性的 AMPARs 正向变构调节剂。AMPA 受体调节剂-9 在人和大鼠模型中选择性地增强 AMPAR 活性,在大鼠胚胎皮层原代神经元中的 EC2x 值为 0.96 μM。AMPA 受体调节剂-9 上调大鼠原代皮层神经元培养物中的 BDNF 蛋白表达。AMPA 受体调节剂-9 增强大鼠和小鼠中 AMPA 介导的兴奋性突触后反应。AMPA 受体调节剂-9 可用于认知障碍研究。

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AMPA receptor modulator-9

AMPA receptor modulator-9 Chemical Structure

CAS No. : 1204572-46-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AMPA receptor modulator-9 is an orally active, selective positive allosteric modulator (PAM) of AMPARs with blood-brain barrier penetration. AMPA receptor modulator-9 selectively potentiates AMPAR activity in human and rat models, with an EC2x value of 0.96 μM in rat embryonic cortex primary neurons. AMPA receptor modulator-9 upregulates BDNF protein expression in rat primary cortical neuronal cultures. AMPA receptor modulator-9 enhances AMPA-mediated excitatory postsynaptic responses in rat and mice. AMPA receptor modulator-9 can be used for the study of cognitive disorders[1].

IC50 & Target[1]

AMPA Receptor

 

体外研究
(In Vitro)

AMPA receptor modulator-9 (Compound 14o) 在大鼠胚胎皮层原代神经元培养物中发挥 AMPA 受体增强活性,其 EC2x 值为 0.96 μM[1]
AMPA receptor modulator-9 增强注射了大鼠皮层或人海马 poly(AM+) mRNA 的非洲爪蟾卵母细胞中 AMPA 诱发的内向电流 (大鼠皮层 mRNA:EC50 = 9.9 μM;人海马 mRNA:EC50 = 18 μM)[1]
AMPA receptor modulator-9 (3-30 μM) 通过增强反应面积调节大鼠海马切片 CA1 区域中 AMPA 介导的兴奋性突触后反应[1]
AMPA receptor modulator-9 (0.3-10 μM, 24 h) 以剂量依赖方式上调大鼠原代皮层神经元培养物中的 BDNF 蛋白表达[1]

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

体内研究
(In Vivo)

AMPA receptor modulator-9 (Compound 14o) (0.01-30 mg/kg,腹腔注射,单次给药) 显著增强麻醉大鼠齿状回中长期增强的诱导和维持[1]

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

Animal Model: Adult Wistar rats, Adult CD1 mice and Adult C57BI/6 mice[1]
Dosage: 0.01, 0.03, 1, 3, 10, 30 mg/kg
Administration: i.p., single dose
Result: Enhanced the induction and maintenance of long-term potentiation (LTP) in the dentate gyrus (10, 30 mg/kg).
Improved episodic memory in CD1 mice (1, 3 mg/kg).
Enhanced spatial working memory in C57BI/6 mice (0.01, 0.03 mg/kg).
Exertd neuroprotective effects in Wistar rats with transient global cerebral ischemia (10mg/kg).
分子量

293.17

Formula

C10H10Cl2N2O2S

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
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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.

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产品名称:
AMPA receptor modulator-9
目录号:
HY-178153
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