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

Eticlopride 是一种选择性多巴胺 D2 样受体拮抗剂,对多巴胺 D2、α1-肾上腺素能、α2-肾上腺素能、5HT1、5HT2 受体具有高亲和力,Ki 分别为 0.09、112、699、6220 和 830 nM。Eticlopride 具有抗精神疾病的作用。

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Eticlopride

Eticlopride Chemical Structure

CAS No. : 84226-12-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Eticlopride, a selective dopamine D2‐like receptor antagonist, exhibits high affinity for dopamine D2, α1‐adrenergic, α2‐adrenergic, 5HT1, 5HT2 receptors with Kis of 0.09, 112, 699, 6220, and 830 nM, respectively. Eticlopride is an antipsychotic agent[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]
体外研究
(In Vitro)

Eticlopride (1 μM, 6 h) 可消除 DA 的作用,而 DA 可增加 HUVEC 细胞中的 KLF2 表达[2]
Eticlopride (1 μM,15 分钟) 可消除大鼠纹状体神经元中 D2R/SSTR2 的异二聚化[3]

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

体内研究
(In Vivo)

Eticlopride (10 mg/kg,腹腔注射) hydrochloride 阻断了原位 PC3 和 HT29 肿瘤动物中 DA 恢复的正常血管形态[2]
Eticlopride (0.01 或 0.02 mg/kg,腹腔注射) hydrochloride 可缓解大鼠中 Quinpirole (HY-B1752) 引起的认知缺陷[4]

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

Animal Model: Sprague-Dawley rats treated with Ruinpirole (1 mg/kg) from postnatal days 1 to 21[4]
Dosage: 0.01 or 0.02 mg/kg
Administration: i.p.
Result: Alleviated cognitive deficits produced by neonatal quinpirole treatment in both male and female rats on the place version of the MWT, as well as in males tested on the match-to-place version of the MwT (MwT tested on P22 to P28).
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
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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.

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产品名称:
Eticlopride
目录号:
HY-121129
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