2. GPCR/G Protein Neuronal Signaling
  3. mGluR
  4. ADX88178 TFA

ADX88178 TFA 是一种具有口服活性的、血脑屏障穿透性的、选择性 mGluR4 正向变构调节剂，对 hmGluR4 的 EC50 为 3.5 nM。ADX88178 TFA 可调节 mGlu4 活性，增强谷氨酸介导的受体激活作用，提高谷氨酸对受体的表观亲和力。ADX88178 TFA 可逆转氟哌啶醇诱导的僵住症，增强左旋多巴 (L-DOPA) 和喹吡罗的作用，但无法减轻已形成的异常不自主运动，不会加重左旋多巴诱导的运动障碍，且单独使用时不影响前肢运动不能症状。ADX88178 TFA 可用于左旋多巴诱导的运动障碍和帕金森病的相关研究。

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ADX88178 TFA

ADX88178 TFA Chemical Structure

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ADX88178 TFA 的其他形式现货产品:

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ADX88178 TFA 相关抗体

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MCE 顾客使用本产品发表的 1 篇科研文献

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ADX88178 TFA is an orally active, blood-brain barrier-penetrant, selective positive allosteric modulator of mGluR4, with an EC50 of 3.5 nM against hmGluR4. ADX88178 TFA modulates mGlu4 activity, enhances glutamate-mediated receptor activation, and increases the apparent affinity of glutamate for the receptor. ADX88178 TFA reverses haloperidol-induced catalepsy, potentiates the effects of levodopa (L-DOPA) and quinpirole, but fails to alleviate established abnormal involuntary movements, does not exacerbate L-DOPA-induced dyskinesia, and does not affect forelimb akinesia when administered alone. ADX88178 TFA can be used in research related to L-DOPA-induced dyskinesia and Parkinson's disease[1][2].

IC50 & Target[1]

hmGluR4

3.5 nM (EC50)

体外研究
(In Vitro)

ADX88178(30 nM-3 μM) TFA 可强效增强表达 hmGluR4 的 HEK293 细胞中谷氨酸介导的钙动员，其 EC50 为 3.5 nM，且无固有激动剂活性[2]。
ADX88178 TFA 可增强表达大鼠 mGluR4 的 HEK293 细胞中谷氨酸介导的钙动员，其 EC50 为 9.1 nM，且无固有激动剂活性[2]。
ADX88178 TFA 对细胞色素 P450 酶具有不同强度的抑制作用，其中对 CYP1A2 的抑制作用最强 (IC50 = 0.46 μM)，对 CYP2D6 的抑制作用较弱 (IC50 >50 μM)[2]。
ADX88178 (1000 ng/mL) TFA 血浆蛋白结合率较低，在大鼠血浆中的游离分数为 8.1%，小鼠血浆中为 21.5%[2]。

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

ADX88178 TFA 相关抗体:
体内研究
(In Vivo)

ADX88178 (10-30 mg/kg；口服) TFA 无法减轻 6-羟基多巴胺损伤大鼠中预先形成的 L-DOPA 诱导的异动症[1]。
ADX88178 (0.1-10 mg/kg；口服) TFA 可剂量依赖性逆转氟哌啶醇诱导的雄性 Sprague-Dawley 大鼠僵住症，其 ED50 为 1.1 mg/kg，在 3 和 10 mg/kg 剂量下可观察到显著效应[2]。
ADX88178 (3-30 mg/kg；口服；10 mg/kg；腹腔注射) TFA 单独使用无法改善 6-OHDA 损伤雄性 Sprague-Dawley 大鼠的前肢运动不能症状，但它可剂量依赖性地增强亚最大剂量 L-DOPA 的疗效，当 ADX88178 剂量为 30 mg/kg 联合 6 mg/kg L-DOPA 时，可完全逆转运动缺陷[2]。

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

Animal Model: Sprague-Dawley (male, 270-300 g, 6-hydroxydopamine-lesioned, primed with L-DOPA + benserazide to establish stable AIMs)[1]
Dosage: 10 mg/kg; 30 mg/kg
Administration: p.o.; single dose 30 min prior to L-DOPA + benserazide
Result: Failed to produce a significant reduction in total AIMs scores compared to vehicle.
Failed to produce significant effects on axial, forelimb, or orolingual AIMs subtypes.
Animal Model: Sprague-Dawley (male, 260-450 g, haloperidol-induced catalepsy)[2]
Dosage: 0.1 mg/kg; 0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: p.o.
Result: Produced a dose-dependent reversal of catalepsy.
Reduced catalepsy latency to 33.4 seconds (a 62.3% reduction from haloperidol alone) at 3 mg/kg.
Reduced catalepsy latency to 25.7 seconds (a 71.0% reduction from haloperidol alone) at 10 mg/kg.
Achieved an ED50 of 1.1 mg/kg for catalepsy reversal.
Reached an in vivo plasma EC50 of 92 ng/mL (338 nM).
Animal Model: Sprague-Dawley (male, 225-300 g, bilateral striatal 6-hydroxydopamine lesions)[2]
Dosage: 3-30 mg/kg (p.o.); 10 mg/kg (i.p.)
Administration: p.o.; i.p.;
Result: Showed no significant effect on forelimb stepping scores when administered alone at 3, 10, or 30 mg/kg p.o.
Increased forelimb steps to ~18 when coadministered with 6 mg/kg L-DOPA at 3 mg/kg p.o.
Increased forelimb steps to ~23 when coadministered with 6 mg/kg L-DOPA at 10 mg/kg p.o.
Fully reversed forelimb stepping deficit, restoring steps to pre-lesion levels (~35) when coadministered with 6 mg/kg L-DOPA at 30 mg/kg p.o.
Potentiated L-DOPA efficacy at 10 mg/kg i.p., allowing full reversal of akinesia at 60 mg/kg L-DOPA (vs. 120 mg/kg L-DOPA alone).
分子量

386.35

Formula

C14H13F3N6O2S
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

ADX88178 TFA 相关分类

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  • 稀释计算器

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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.

Keywords:

ADX88178ADX 88178ADX-88178mGluRMetabotropic glutamate receptorshumanL-DOPA-induced dyskinesiacytochrome P450 enzymesratSprague-Dawley ratsmGluR46-hydroxydopamine-lesioned ratsParkinson’s diseaseHEK293 cellsglutamateInhibitorinhibitorinhibit

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