2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor
  4. PD-168077

PD-168077 是一个选择性的多巴胺 D4 受体激动剂，其 Ki 值为 9 nM。

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PD-168077 Chemical Structure

PD-168077 Chemical Structure

CAS No. : 190383-31-4

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PD-168077 的其他形式现货产品:

Other Forms of PD-168077:

PD-168077 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:

查看所有亚型
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

PD-168077 is a selective dopamine D4 receptor agonist, with a Ki of 9 nM[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO EC50
17 nM
Compound: 6
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
[PMID: 9191952]
HEK293 EC50
> 10 μM
Compound: 2
Agonist activity at human recombinant D2 receptor expressed in HEK293 cells by FLIPR assay
Agonist activity at human recombinant D2 receptor expressed in HEK293 cells by FLIPR assay
[PMID: 16913699]
HEK293 IC50
> 10 μM
Compound: 2
Antagonist activity at human recombinant D2 receptor expressed in HEK293 cells by FLIPR assay
Antagonist activity at human recombinant D2 receptor expressed in HEK293 cells by FLIPR assay
[PMID: 16913699]
HEK293 EC50
8.3 nM
Compound: 2, PD-168077
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
[PMID: 17149874]
HEK293 EC50
8.3 nM
Compound: 2
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
[PMID: 16913699]
体外研究
(In Vitro)

PD-168077 是最早被确定为选择性 D4 激动剂的药物之一。它比 D2 样受体家族的其他成员及其 D1 样受体显示出 >100 倍的选择性；PD-168077 对 α1 和 α2 的选择性是 20 倍，对 5-HT1A 的选择性是 45 倍，并且选择性是 5-HT2A 受体的 460 倍；PD-168077 证明 D4 受体在 CHO 细胞中类似喹吡罗抑制毛喉素刺激的 cAMP 积累或刺激[3H]胸苷摄取方面的内在活性表达人类 D4 受体[1]。在 PD-168077 处理的细胞中，p-CaMKII 在突触位点表现出显著增加的聚集，如与 PSD-95增强的共定位所示[2]。

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

PD-168077 相关抗体:
体内研究
(In Vivo)

PD-168077 (0.2-25.0 mg/kg) 以剂量依赖的方式诱导运动，这种运动形式不寻常且具有特征性的“拖步”，伴随着不协调的动作、打哈欠和阵发性肌阵挛；梳理和抬头行为减少[1]。

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

334.41

Formula

C20H22N4O
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

PD-168077 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

PD-168077190383-31-4PD168077PD 168077Dopamine ReceptorInhibitorinhibitorinhibit

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