2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor Arrestin
  4. D1/D5 Receptor agonist-1

D1/D5 Receptor agonist-1 是一种具有血脑屏障通透性并且具有口服活性的 D1/D5 受体 (D1/D5 receptor) 激动剂。D1/D5 Receptor agonist-1 在 cAMP 途径和 β-arrestin 募集方面保持显著疗效，其 EC50 值分别为 3.7 nM (D1R cAMP)、91 nM (D1R β-arrestin)、129 nM (D1R 内化)，对 D1R 结合亲和力的 Ki 值为 111 nM。D1/D5 Receptor agonist-1 在大鼠中抑制 L-DOPA (HY-N0304) 诱导的运动障碍中的 β-arrestin 信号传导。D1/D5 Receptor agonist-1 可用于帕金森病的研究。

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D1/D5 Receptor agonist-1

D1/D5 Receptor agonist-1 Chemical Structure

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D1/D5 Receptor agonist-1 相关抗体

Top Publications Citing Use of Products

查看 Dopamine Receptor 亚型特异性产品:

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Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

查看 Arrestin 亚型特异性产品:

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Arrestin-2/β-Arrestin 1 Arrestin-3/β-Arrestin 2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

D1/D5 Receptor agonist-1 is a highly brain-penetrant and orally active D1/D5 receptor agonist. D1/D5 Receptor agonist-1 maintains considerable efficacy in the cAMP pathway and in β-arrestin recruitment, with EC50s of 3.7 nM (D1R cAMP), 91 nM (D1R β-arrestin), 129 nM (D1R internalization) and a Ki of 111 nM (D1R binding affinity). D1/D5 Receptor agonist-1 inhibits β-arrestin signaling in a rat with L-DOPA (HY-N0304) induced dyskinesias. D1/D5 Receptor agonist-1 can be used for the study of Parkinson’s disease[1].

IC50 & Target[1]

D1 Receptor

 

D5 Receptor

 

体外研究
(In Vitro)

D1/D5 Receptor agonist-1 (Compound 24) (10-4-10 μM) 在 cAMP 途径和 β-arrestin 蛋白募集方面保持显著疗效，其 EC50 值分别为 3.7 nM (D1R cAMP)、91 nM (D1R β-arrestin)、129 nM (D1R 内化) ，对 D1R 结合亲和力的 Ki 值为 111 nM[1]。

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

D1/D5 Receptor agonist-1 相关抗体:
体内研究
(In Vivo)

D1/D5 Receptor agonist-1 (Compound 24) (0.3-3 mg/kg，口服，单次给药) 在 L-DOPA (HY-N0304) 诱导的帕金森病大鼠异动症模型中抑制 β-arrestin 信号传导[1]。

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

Animal Model: 6-OHDA and L-DOPA (HY-N0304)-induced dyskinesias in adult male SD rats (180 g)[1]
Dosage: 0.3, 1, 3 mg/kg
Administration: p.o. for a single dose
Result: Decreased EEG beta power over a longer time course (up to 4 h).
Showed comparable efficacy to a therapeutic dose of L-DOPA and with significantly fewer concomitant dyskinesias at doses with predicted D1 RO of 30 to 50%.
分子量

368.32

Formula

C18H13FN4O4
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

D1/D5 Receptor agonist-1 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

D1/D5 Receptor agonist-1Dopamine ReceptorArrestinD1/D5 receptorParkinson’s disease,β-arrestinInhibitorinhibitorinhibit

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