1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. iGluR
  3. GluN2B-NMDAR Allosteric modulator 1

GluN2B-NMDAR Allosteric modulator 1 是一种选择性 GluN2B-NMDAR 正向变构调节剂。GluN2B-NMDAR Allosteric modulator 1 可增强谷氨酸和天冬氨酸诱发的 GluN2B-NMDAR 门控电流,其 EC50 值分别为 43.7 nM 和 18 nM。GluN2B-NMDAR Allosteric modulator 1 可逆转小鼠的焦虑样行为和社会认知缺陷。GluN2B-NMDAR Allosteric modulator 1 可用于神经系统疾病的研究,如焦虑症 。

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GluN2B-NMDAR Allosteric modulator 1

GluN2B-NMDAR Allosteric modulator 1 Chemical Structure

CAS No. : 2419700-58-4

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  • 生物活性

  • 纯度 & 产品资料

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生物活性

GluN2B-NMDAR Allosteric modulator 1 is a selective GluN2B-NMDAR positive allosteric modulator. GluN2B-NMDAR Allosteric modulator 1 can increase glutamate- and aspartate-evoked GluN2B-NMDAR-gated currents with EC50 values of 43.7 and 18 nM. GluN2B-NMDAR Allosteric modulator 1 can reverse anxiety-like behavior and social cognition deficits in mice. GluN2B-NMDAR Allosteric modulator 1 can be used for the research of neurological disease, such as anxiety[1].

IC50 & Target[1]

GluN2B

 

体外研究
(In Vitro)

GluN2B-NMDAR Allosteric modulator 1 (Compound 175) (0.001-100 μM) 可升高 HEK293 细胞中谷氨酸诱导的 GluN1/GluN2B-NMDAR 门控电流,其 EC50 为 43.7 nM (logEC50 = -7.36)[1]
GluN2B-NMDAR Allosteric modulator 1 (0.0001-1 μM) 可在原代大鼠海马神经元中呈剂量依赖性且选择性地增强天冬氨酸诱发的含 GluN2B 的天然 NMDAR 电流,其 EC50 为 18 nM[1]
GluN2B-NMDAR Allosteric modulator 1 (1 μM;3 h) 不会在原代皮质神经元中诱导细胞毒性[1]

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

体内研究
(In Vivo)

GluN2B-NMDAR Allosteric modulator 1 (Compound 175) (1 mg/kg;腹腔注射;突触可塑性诱导前 30 分钟给药) 可通过依赖含 GluN2B 的 NMDAR 的机制,在麻醉大鼠中促进低频刺激诱导的长时程抑郁[1]
GluN2B-NMDAR Allosteric modulator 1 (1 mg/kg;腹腔注射;单次给药) 可逆转 7 月龄 Mecp2-OE 小鼠以及携带可诱导表达达 Disc1-N 的转基因小鼠品系的焦虑样行为与社会认知缺陷[1]

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

Animal Model: Mecp2-OE mice (7 months old); a transgenic mouse line harboring an inducible expression of Disc1-N mice (C57BL/6; 3-4 months old) [1]
Dosage: 1 mg/kg
Administration: I.p.; single dose (30 minutes before each behavioral test)
Result: Restored center time in the open-field test to WT levels (reversing anxiety-like behavior) and significantly improved social preference index in Mecp2-OE mice.
Increased time spent in the center of the open-field test (reversing anxiety-like behavior), increased spontaneous alternation in the Y-maze test (improving spatial working memory) and increased social preference index in the three-chamber test (reversing sociability deficit) in Disc1-N mice.
分子量

295.38

Formula

C17H21N5

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.

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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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GluN2B-NMDAR Allosteric modulator 1
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