2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR
  4. R-(+)-EU-1180-453

R-(+)-EU-1180-453 是靶向含 GluN2C 和 GluN2D 亚基的 NMDA 受体的阳性调节剂，对大鼠两种受体亚型的 pEC50 值均为 5.5，且可穿过血脑屏障。R-(+)-EU-1180-453 能够提升谷氨酸的效能，增强受体对最大有效浓度激动剂的反应，且仅作用于结合了两种共激动剂的受体。R-(+)-EU-1180-453 可用于阿尔茨海默病、帕金森病、癫痫、神经性疼痛相关研究。

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R-(+)-EU-1180-453

R-(+)-EU-1180-453 Chemical Structure

CAS No. : 2488764-06-1

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R-(+)-EU-1180-453 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

R-(+)-EU-1180-453 is a positive allosteric modulator targeting NMDA receptors containing GluN2C and GluN2D subunits, with a pEC50 value of 5.5 for both rat receptor subtypes, and it can cross the blood-brain barrier. R-(+)-EU-1180-453 increases the potency of glutamate, enhances receptor responses to maximally effective concentrations of agonists, and acts only on receptors bound to both co-agonists. R-(+)-EU-1180-453 is applicable to research related to Alzheimer's disease, Parkinson's disease, epilepsy, and neuropathic pain[1].

体外研究
(In Vitro)

R-(+)-EU-1180-453 (30 μM; concentrations for concentration−effect curves) 可增强在非洲爪蟾卵母细胞中表达的 GluN1/GluN2C 和 GluN1/GluN2D NMDA 受体，其 pEC50 为 5.5，最大增强幅度分别为 410% 和 390%，p (doubling concentration) 分别为 5.9 和 5.8[1]。

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

R-(+)-EU-1180-453 相关抗体:
体内研究
(In Vivo)

EU-1180-453 (10 mg/kg；腹腔注射；单剂量) 可穿透雄性 C57BL/6 小鼠的血脑屏障，在单次 10 mg/kg 腹腔注射给药后，其脑与血浆的 AUC0-t 比值达 1.4，血浆半衰期为 1.07 hours[1]。

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

Animal Model: C57BL/6 (male, 6-8 weeks of age, fed)[1]
Dosage: 10 mg/kg
Administration: i.p.; single dose
Result: Reached peak plasma concentration of 695 ng/mL (1.83 μM) at 0.25 hours post-dosing.
Reached peak brain concentration of 962 ng/mL (2.5 μM) at 0.25 hours post-dosing.
Achieved a brain:plasma AUC_LAST ratio of 1.4.
Exhibited a plasma half-life (t1/2) of 1.07 hours.
Showed plasma protein binding of 98.7% bound at 1 μM, with 1.3% free fraction.
分子量

380.42

Formula

C22H21FN2O3
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

R-(+)-EU-1180-453 相关分类

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Keywords:

R-(+)-EU-1180-4532488764-06-1iGluRIonotropic glutamate receptorsschizophreniaepilepsyhuntington’s choreaXenopus laevis oocytesmale C57BL/6 miceNMDA receptorsGluN2C-containing NMDA receptorsparkinson’s diseaseGluN2D-containing NMDA receptorsalzheimer’s diseaseInhibitorinhibitorinhibit

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