2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR
  4. NMDA receptor modulator 9

NMDA receptor modulator 9 是一种具有口服活性的 NMDA 受体正变构调节剂 (PAM)。NMDA receptor modulator 9 增强 GluN2A 受体活性。NMDA receptor modulator 9 在慢性束缚应激 (CRS) 诱导的抑郁小鼠模型中表现出显著的抗抑郁样作用。NMDA receptor modulator 9 可用于抑郁症的研究。

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NMDA receptor modulator 9

NMDA receptor modulator 9 Chemical Structure

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NMDA receptor modulator 9 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NMDA receptor modulator 9 is an orally active NMDA receptor positive allosteric modulator (PAM). NMDA receptor modulator 9 enhances GluN2A receptor activity. NMDA receptor modulator 9 demonstrates significant antidepressant-like effects in chronic restraint stress (CRS)-induced depression mice. NMDA receptor modulator 9 can be used for the study of depression[1].

体外研究
(In Vitro)

NMDA receptor modulator 9 (Compound Y36) (30 μM) 仅在与谷氨酸和甘氨酸 (Glycine) (HY-Y0966) 共同给药时，显著增强表达 GluN1/GluN2A 的非洲爪蟾卵母细胞中 GluN2A 受体介导的电流[1]。
NMDA receptor modulator 9 显示出比 GNE-3419 (Emax = 196.4%) 更高的效能 (Emax = 397.7%)，降低了 GluN2A 受体上 glutamate/Glycine 的EC50 值并增加了 Emax 值[1]。
NMDA receptor modulator 9 (200 μM) 在 HEK293、PC12 和 SH-SY5Y 细胞系中未表现出显著的细胞毒性[1]。
NMDA receptor modulator 9 对 hERG 通道的亲和力较弱，IC50 为 67.85 μM，表明其心脏毒性风险低[1]。

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

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

NMDA receptor modulator 9 (Compound Y36) (0.1-1.0 mg/kg，腹腔给药或口服给药，单次给药) 缓解慢性束缚应激 (CRS) 小鼠的抑郁相关行为[1]。
NMDA receptor modulator 9 (Compound Y36) (200-350 mg/kg，口服给药，单次给药) 在雄性 C57BL/6J 小鼠中表现出缓慢的死亡率，LD50 为 270.82 mg/kg[1]。
NMDA receptor modulator 9 (0.3-1.0 mg/kg，腹腔给药，每 2 天给药一次，持续 30 天) 在 ICR 小鼠中未引起异常行为，体重稳定，器官/体重比无显著变化，且无明显的肾毒性、肝毒性或心肌损伤[1]。

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

Animal Model: C57BL/6J mice (subjected to 4 h daily restraint stress for 28 days)[1]
Dosage: 0.1, 0.3, 1.0 mg/kg
Administration: i.p. or p.o.for a single dose
Result: Increased central area entries in OFT.
Reduced immobility time in TST.
Enhanced sucrose preference in SPT (alleviating anhedonia).
分子量

373.44

Formula

C19H20FN3O2S
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

NMDA receptor modulator 9 相关分类

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  • 稀释计算器

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Help & FAQs
  • 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:

NMDA receptor modulator 9NMDA receptor modulator9NMDA receptor modulator-9iGluRIonotropic glutamate receptorsNMDA receptorpositive allosteric modulatorchronic restraint stressdepressionInhibitorinhibitorinhibit

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