2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR
  4. JNJ-78911118

JNJ-78911118 是一种强效、可穿透血脑屏障的选择性 GluN2A 拮抗剂 (IC50 = 44 nM)。JNJ-78911118 对 GluN1/2B、2C 和 2D 受体的选择性超过 200 倍。JNJ-78911118 作为一种负性变构调节剂 (NAM)，能够显著抑制谷氨酸在 GluN1/2A 受体上的效力并降低甘氨酸的效力。JNJ-78911118 在体内产生显著的药效学效应。JNJ-78911118 可用于抑郁症的相关研究。

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JNJ-78911118

JNJ-78911118 Chemical Structure

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JNJ-78911118 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

JNJ-78911118 is a potent, brain-penetrant, selective GluN2A antagonist (IC50 = 44 nM). JNJ-78911118 shows >200-fold selectivity against GluN1/2B, 2C and 2D receptors. JNJ-78911118 functions as a negative allosteric modulator (NAM) by insurmountably suppressing glutamate efficacy and reducing glycine potency at GluN1/2A receptors. JNJ-78911118 produces profound pharmacodynamic effects in vivo. JNJ-78911118 can be used for depression research[1].

IC50 & Target[1]

GluN2A

44 nM (IC50)

体外研究
(In Vitro)

JNJ-78911118 (10 pM-10 μM，2 小时) 以浓度依赖的方式置换海马神经元膜上与放射性配体 JNJ-74950343 结合的 GluN1/2A 界面，不改变谷氨酸的效力，但降低其对同源 GluN1/2A 受体的活性[1]。
JNJ-78911118 (10 μM，24-72 小时) 促进大鼠海马神经元培养物中神经突的生长和突触的形成，并在 72 小时后显著增强树突复杂性的多种指标[1]。
JNJ-78911118 (1-10 μM) 在包含 77 个离子通道、受体和转运体的定制筛选面板以及一个包含 373 个激酶的面板中，对所有靶点均显示出低于 50 % 的抑制率[1]。

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

JNJ-78911118 相关抗体:
体内研究
(In Vivo)

JNJ-78911118 (60 mg/kg，皮下注射，单次给药) 可减轻弗氏完全佐剂 (CFA，HY-153808) 诱导的炎症性疼痛小鼠模型中的机械性痛觉过敏，可抑制大鼠海马长时程增强作用，并增加大鼠前额叶皮层的微型兴奋性突触后电流 (mEPSC) 频率[1]。
JNJ-78911118 (50 和 250 mg/kg，口服，每日两次，连续 4 天或同一天两次) 在大鼠中总体耐受性良好，但会产生剂量相关的血流动力学效应[1]。

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

Animal Model: Male C57BL/6 N mice (8-12 weeks)[1]
Dosage: 60 mg/kg
Administration: s.c., single dose 2 days post-CFA
Result: Partly reversed CFA induced allodynia at 60 mg/kg, while Gabapentin (HY-A0057, 150 mg/kg, p.o.) completely reversed it.
Reduced tactile allodynia at 30 min and 1 h post-administration compared to controls.
Had no effect on paw withdrawal thresholds (PWTs) 24 h post-dosing.
Animal Model: Wild-type C57BL/6J and homozygous Grin2a KO mice[1]
Dosage: 60 mg/kg
Administration: s.c., single dose 2 days post-CFA
Result: Mitigated CFA-induced allodynia in wild type mice at 30 min and 1-h post-administration.
Did not significantly reduce CFA-induced mechanical allodynia in Grin2a KO mice.
Animal Model: Male Sprague-Dawley rats (8-10 weeks)[1]
Dosage: 60 mg/kg
Administration: s.c., single dose 30 min pre-TBS
Result: Did not alter baseline synaptic transmission but completely blocked the induction of LTP by theta burst stimulation (TBS).
The population spike amplitude remained at pre-stimulation levels throughout the recording period (50-60 min post-TBS).
Animal Model: Male Sprague-Dawley rats (6-10 weeks)[1]
Dosage: 60 mg/kg
Administration: s.c., single dose (24 h before recording)
Result: Induced a significant decrease in the inter-event interval of mEPSCs in layer 5 pyramidal neurons in rat medial prefrontal cortex.
Showed no significant changes in mEPSC amplitude.
Animal Model: Male Wistar Han rats [1]
Dosage: 50 and 250 mg/kg
Administration: p.o., twice daily for 4 days
Result: Achieved dose-dependent plasma exposures, with Cmax and AUC increasing less than dose proportionally (80 and 180 %, respectively, and Tmax occurring 1-3 h post-dose.
Minimal activity decreases or minimal hypoactivity were observed 2 h post-dose on days 1-3.
Piloerection was observed in high-dose animals on Day 1 at 3 h post-dose.
Low doses had no effect on body weight, while the high dose caused a transient 3 % decrease in two animals and lower overall body weight gain in all animals.
No meaningful changes were detected in globulin, protein, albumin, chloride, calcium and potassium concentrations, cholesterol level or reticulocyte count.
Produced mild decreases in triglyceride levels.
Showed no Olney's lesions in animals.
Animal Model: Male Sprague-Dawley rats (8-10 weeks)[1]
Dosage: 50 and 250 mg/kg
Administration: p.o., twice on the same day
Result: The low dose increased heart rate and mean arterial pressure.
The high dose caused a transient decrease in heart rate (associated with reduced body temperature) and an increase in blood pressure.
分子量

419.81

Formula

C19H16ClF2N5O2
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

JNJ-78911118 相关分类

  • 摩尔计算器

  • 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:

JNJ-78911118JNJ78911118JNJ 78911118iGluRIonotropic glutamate receptorsGluN2ANAMdepressionrat hippocampal neuronalTBSCFAInhibitorinhibitorinhibit

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