2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor
  4. A-77636

A-77636 是一种口服有效的、选择性的长效 多巴胺 D1 受体 激动剂 (pEC50 = 8.13; EC50 = 1.1 nM)。A-77636 对多巴胺 D1 受体显示出最高的亲和力 (pKi = 7.40 ± 0.09；Ki = 39.8 nM)。A-77636 具有抗帕金森病活性。

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A-77636 Chemical Structure

A-77636 Chemical Structure

CAS No. : 778546-51-3

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A-77636 的其他形式现货产品:

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A-77636 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

A-77636 is an orally active, potent, selective and long-acting dopamine D1 receptor agonist (pEC50 = 8.13; EC50 = 1.1 nM). A-77636 shows the highest affinity (pKi = 7.40 ± 0.09; Ki = 39.8 nM) for the dopamine D1 receptor. A-77636 shows antiparkinsonian activity[1].

IC50 & Target

Dopamine D1 receptor

1.1 nM (EC50)

Dopamine D1 receptor

39.8 nM (Ki)

体内研究
(In Vivo)

A-77636 (0-3.2 μmol/kg，皮下注射) 在 6-OHDA 损伤的大鼠中引发旋转行为(ED50=0.32 μmol/kg sc)[1]。
A-77636 (1-10 mg/kg) 以剂量依赖性方式减弱成瘾剂诱导的运动活动[2]。
A-77636 在大鼠 (ED50=12.3 μmol/kg s.c.) 和小鼠 (ED50=12.1 μmol/kg s.c.) 中产生前肢阵挛[1] 。
在用 MPTP 处理以诱导帕金森样状态的狨猴中，A-77636 (0.5、1.0 或 2.0 μmol/kg，口服)可增加运动活性并降低帕金森样症状的严重程度：该化合物在皮下或口服给药后均有活性[1]。

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

Animal Model: Rats with unilateral 6-OHDA (6-hydroxydopamine) lesions of the nigrostriatal pathway (six/group)[1]
Dosage: 0.32, 1.0, 3.2 μmol/kg
Administration: Subcutaneously
Result: Elicited prolonged (> 20 h) contralateral turning, which was blocked by SCH 23390, a D1 receptor antagonist, but not by haloperidol at doses selective for the dopamine D2 receptor.
Animal Model: Male Swiss Webster mice (18-25 g, five or six per cage)[2]
Dosage: 1, 3, 10 mg/kg
Administration:
Result: Attenuated addiction-induced locomotor activity in a dose-dependent manner. When administered alone, 1 and 3 mg/kg A-77636 produced little change in locomotor activity, whereas 10 mg/kg produced a significant and substantial decrease in locomotor activity.
分子量

329.43

Formula

C20H27NO3
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.
纯度 & 产品资料
参考文献

A-77636 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:

A-77636778546-51-3A77636A 77636Dopamine ReceptorAntiparkinsonianParkinson's diseaseorally activeInhibitorinhibitorinhibit

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目录号：
HY-141496
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