2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor
  4. Eticlopride

Eticlopride  (Synonyms: FLB-131)

目录号: HY-121129
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摩尔计算器

Eticlopride 是一种强效且选择性的 D2 受体拮抗剂，在 6-羟基多巴胺诱导的广泛多巴胺失神经支配的大鼠中进行了研究。在 21 天内每天注射Eticlopride 会增加完整脑区 D2 受体密度，但不会进一步增加失神经支配区域已经增加的密度。尽管受体密度发生变化，但功能敏感性仍然明显，如在洗脱期由 D2 激动剂喹吡罗诱导的对侧旋转所示。该研究表明，慢性 D2 受体阻滞和多巴胺失神经支配可能在上调 D2 受体密度方面具有共同的机制，这与先前报告的失神经支配和拮抗剂治疗的附加效应相反。

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Eticlopride Chemical Structure

Eticlopride Chemical Structure

CAS No. : 84226-12-0

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Eticlopride 的其他形式现货产品:

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Eticlopride 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Eticlopride, a potent and selective D2 receptor antagonist, was investigated in rats with extensive dopamine denervation induced by 6-hydroxydopamine. Daily injections of eticlopride over 21 days increased D2 receptor density in intact brain regions but did not further augment already increased densities in denervated areas. Despite receptor density changes, functional sensitivity remained evident, as shown by contralateral rotations induced by D2 agonist quinpirole during wash-out periods. The study suggests that chronic D2 receptor blockade and dopamine denervation may share a common mechanism in upregulating D2 receptor density, contrary to previous reports suggesting additive effects of denervation and antagonist treatment[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK-293T IC50
> 10000 nM
Compound: Eticlopride
Antagonist activity at DRD2 (unknown origin) expressed in HEK293T cells transfected with Galphai1-RLuc8 and gamma2-GFP10 assessed as inhibition of quinpirole-induced Gi1 activation pre-incubated with quinpirole for 10 mins before compound incubation for 1
Antagonist activity at DRD2 (unknown origin) expressed in HEK293T cells transfected with Galphai1-RLuc8 and gamma2-GFP10 assessed as inhibition of quinpirole-induced Gi1 activation pre-incubated with quinpirole for 10 mins before compound incubation for 1
[PMID: 27933960]
分子量

340.85

Formula

C17H25ClN2O3
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

Eticlopride 相关分类

  • 摩尔计算器

  • 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:

Eticlopride84226-12-0FLB-131FLB131FLB 131Dopamine ReceptorInhibitorinhibitorinhibit

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