2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor 5-HT Receptor Adrenergic Receptor
  4. NRA-0562

NRA‑0562 是一种多巴胺 (dopamine) 拮抗剂，对 dopamine D1/D2/D3/D4、5‑HT2A 和 α1-肾上腺素受体 (α1‑adrenoceptors) 具有高亲和力。NRA-0562 可呈剂量依赖性逆转药物诱导型大鼠模型中 A9 和 A10 中脑多巴胺神经元放电活动抑制，对 A10 神经元的效力更强 (ED50 = 0.3 mg/kg)。NRA-0562 可升高大鼠伏隔核和背外侧纹状体中的 Fos 样免疫反应性。NRA-0562 可用于精神分裂症的临床前研究。

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NRA-0562

NRA-0562 Chemical Structure

CAS No. : 244276-65-1

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NRA-0562 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

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5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

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α adrenergic receptor β adrenergic receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NRA‑0562 is a dopamine antagonist with high affinities for dopamine D1/D2/D3/D4, 5‑HT2A and α1‑adrenoceptors. NRA-0562 dose‑dependently reverses induced suppression of firing activity in rat A9 and A10 midbrain dopamine neurons, with preferential potency at A10 neurons (ED50 = 0.3 mg/kg). NRA-0562 elevates Fos-like immunoreactivity in rat nucleus accumbens and dorsolateral striatum. NRA-0562 can be used for preclinical research on schizophrenia[1].[1].

IC50 & Target[1]

Human D1 Receptor

7.09 nM (Ki)

Human D2 Receptor

2.49 nM (Ki)

Human D3 Receptor

3.48 nM (Ki)

Human D4 Receptor

1.79 nM (Ki)

α1-adrenergic receptor

 

5-HT2A Receptor

 

体外研究
(In Vitro)

NRA-0562 对人源克隆多巴胺 D1、D2、D3 和 D4 受体具有高结合亲和力，其中对 D4 受体的亲和力最高 (Ki = 1.79 nM)，对 D1 受体的亲和力最低 (Ki = 7.09 nM)[1]。

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

NRA-0562 相关抗体:
体内研究
(In Vivo)

NRA‑0562 (0.1-1 mg/kg，静脉注射，每 2-3 分钟依次给药) 可呈剂量依赖性逆转诱导型大鼠模型的 A9 和 A10 多巴胺神经元放电活动的抑制作用，且对 A10 神经元的效力 (ED50 = 0.3 mg/kg) 比对 A9 神经元 (ED50 = 0.9 mg/kg) 高 3 倍[1]。
NRA-0562 (腹腔注射，1-30 mg/kg) 可剂量依赖性地增加大鼠伏隔核和背外侧纹状体中的 Fos 样免疫反应性，其阳性非典型指数符合非典型抗精神病活性特征[1]。

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

Animal Model: Wistar (male, 300-400 g, electrophysiological studies, methamphetamine-induced dopamine neuron inhibition model)[1]
Dosage: 0.1 ; 0.2 ; 0.7 ;1 mg/kg
Administration: i.v.; sequentially every 2-3 minutes
Result: Reversed methamphetamine-induced inhibition of A9 and A10 dopamine neurons dose-dependently and significantly.
Achieved ED50 values of 0.3 mg/kg (A10) and 0.9 mg/kg (A9) for reversing dopamine neuron inhibition.
Showed no apparent effect on baseline firing rates of A9 or A10 dopamine neurons at 0.1-1 mg/kg.
Animal Model: Wistar (male, 280-320 g, immunohistochemical studies)[1]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration: i.p.
Result: Increased Fos-like positive nuclei counts in the nucleus accumbens and dorsolateral striatum dose-dependently and significantly at all tested doses.
分子量

466.55

Formula

C25H24F2N4OS
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

NRA-0562 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

NRA-0562244276-65-1NRA0562NRA 0562Dopamine Receptor5-HT ReceptorAdrenergic ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorBeta Receptorfunctional dopamine antagonistdopamine D1/D2/D3/D4 receptor5-HT?A receptorα?-adrenoceptormethamphetaminedopamine neuronFos-like immunoreactivityatypical indexratschizophreniaInhibitorinhibitorinhibit

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