2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR
  4. CX1763

CX1763 是一种 AMPAR 变构调节剂。CX1763 可变构增强谷氨酸诱发的电流，加快通道开放，提高含 Glur2 (R) 的 AMPAR 的表面水平。CX1763 增强大鼠海马体中的突触传递。CX1763 可提升大鼠的注意力，并减轻小鼠中安非他明诱导的多动行为。CX1763 可用于注意缺陷多动障碍和阿片类药物诱导的呼吸抑制相关研究。

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CX1763

CX1763 Chemical Structure

CAS No. : 1086378-73-5

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CX1763 相关抗体

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AMPA Receptor NMDA Receptor Kainate Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CX1763 is an AMPAR allosteric modulator. CX1763 allosterically potentiates glutamate-evoked currents, accelerates channel opening, and increases the surface levels of AMPAR containing Glur2 (R). CX1763 enhances synaptic transmission in the rat hippocampus. CX1763 improves attention in rats and attenuates amphetamine-induced hyperactivity in mice. CX1763 can be used in studies related to attention deficit hyperactivity disorder and opioid-induced respiratory depression[1].

IC50 & Target[1]

AMPA Receptor

 

体外研究
(In Vitro)

CX1763 (100 μM) 是大鼠脑细胞膜和神经元中一种低影响型 AMPA 受体正变构调节剂，可增强[3H]AMPA 的结合能力以及谷氨酸诱导的峰值电流，且在浓度高达 100 μM 时无内在激动活性，同时可上调含钙离子不可渗透型 GluR2 (R)的受体[1]。

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

CX1763 相关抗体:
体内研究
(In Vivo)

CX1763 (10 mg/kg；静脉注射；单次) 可在麻醉大鼠中诱导海马体 fEPSP 振幅产生显著且持久的约 20% 增强效应[1]。
CX1763 (1-5 mg/kg；腹腔注射；单次) 在 5 mg/kg 腹腔注射剂量下，可改善大鼠 5CSRTT ADHD 模型中的特定注意力指标 (缩短反应潜伏期、减少提前反应)，同时增加遗漏错误但不改变正确反应率[1]。
CX1763 (1-18 mg/kg；腹腔注射；单次) 可剂量依赖性地降低苯丙胺诱导的小鼠活动亢进，其 AD50 为 2 mg/kg，腹腔注射 18 mg/kg 时可完全逆转该症状[1]。

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

Animal Model: Long-Evans (male, 250-350 g)[1]
Dosage: 10 mg/kg
Administration: i.v.; single dose
Result: Significantly potentiated hippocampal fEPSP amplitude by ~20% at 15 minutes post-dose.
Peaked at ~15 minutes post-dose.
Declined to baseline by 100-120 minutes post-dose.
Animal Model: hooded Wistar (male, 250-310 g, 5-Choice Serial Reaction Time Task trained)[1]
Dosage: 1 mg/kg; 5 mg/kg
Administration: i.p.; single dose
Result: Did not significantly alter 5CSRTT parameters at 1 mg/kg.
Significantly decreased correct response latency at 5 mg/kg.
Significantly decreased the percentage of premature responses at 5 mg/kg.
Significantly increased omission errors at 5 mg/kg.
Did not significantly improve the percentage of correct responses at 5 mg/kg.
Animal Model: CD1[1]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg; 18 mg/kg
Administration: i.p.; single dose
Result: Dose-dependently reduced amphetamine-induced hyperactivity, with an AD50 of 2 mg/kg.
Significantly reduced hyperactivity at doses of 3-18 mg/kg.
Completely reversed amphetamine-induced hyperactivity to baseline levels at 18 mg/kg.
分子量

275.30

Formula

C14H17N3O3
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

CX1763 相关分类

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Keywords:

CX17631086378-73-5CX 1763CX-1763iGluRIonotropic glutamate receptorsratsADHDopioid-induced respiratory depressionrat hippocampiAMPARrat neuronsGlur2(R)-containing AMPARAMPA-glutamate receptormicerat brain membranesInhibitorinhibitorinhibit

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