2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor 5-HT Receptor Adrenergic Receptor
  4. NRA-0160

NRA-0160 是一种选择性的 dopamine D4 receptor 拮抗剂，Ki 值为 0.48 nM；同时对 dopamine D2 receptor，D3 receptor，大鼠 5-HT2A receptor 和 α1 adrenoceptor 分别具有不同程度的亲和度，Ki 值分别为 >10000 nM，39 nM，180 nM 和 237 nM。

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NRA-0160 Chemical Structure

NRA-0160 Chemical Structure

CAS No. : 204718-47-8

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NRA-0160 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-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

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α adrenergic receptor β adrenergic receptor

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

NRA-0160 is a selective dopamine D4 receptor antagonist, with a Ki value of 0.48 nM and with negligible affinity for dopamine D2 receptor (Ki: >10000 nM), D3 receptor (Ki: 39 nM), rat 5-HT2A receptor (Ki: 180 nM) and rat α1 adrenoceptor (Ki: 237 nM).

IC50 & Target

D4 Receptor

0.48 nM (Ki)

D3 Receptor

39 nM (Ki)

5-HT2A Receptor

180 nM (Ki, in rat)

Rat α1 adrenoceptor

237 nM (Ki)

体内研究
(In Vivo)

NRA0160 (0.1, 1, or 3 mg/kg, i.p.) has no effect on PCP-induced hyperlocomotion, stereotypy or ataxia in SD rats. NRA0160, at any dose, does not reduce cumulated counts of locomotion and cumulated scores of stereotypy emerging, and has no effect on extracellular glutamate levels and locomotor activity emerged after saline injection[1]. NRA0160 dose-dependently and significantly reverses the effects of MAP on both A9 and Al0 dopamine neurons. NRA0160 is slightly more potent in reversiig the effects of MAP on A10 (ED50 = 1.0 mg/kg) than on A9 dopamine neurons (ED50 = 1.3 mg/kg). NRA0160 reverses the effect of AP0 on both A9 and A10 dopamine neurons. ED50 values for the effects of NRA0160 on APO-induced inhibition of A9 and A10 dopamine neurons are 1.3 mg/kg and 0.5 mg/kg, respectively[2].

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

439.52

Formula

C24H23F2N3OS
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
Animal Administration
[2]

Methamphetamine (MAP, 1 mg/kg, iv) or apomorphine (APO, 40 μg/kg iv.) and incremental doses of NRA0160 or G745870 (the starting dose is 0.1 mg/kg with sequential doses of 0.2, 0.7 and 2 mg/kg) are administered every 2-3 min (drug-induced changes usually reached their plateaus in 2-3 min) via an i.v. catheter implanted in the femoral vein of rats. Drug-induced changes (after reaching plateau) in neuronal activities which are plotted as percent changes from the preinjection baseline rate, are recorded over a 5 min period and defined as 100%. The % inhibition is calculated and ED50 values are determined. The ED50 values are analyzed by fitting it to the four parametric logistic functions, using non-linear least square regression (-) Apomorphine hydrochloride, methamphetamine HCl and L 745870 3HCl are dissolved in 0.9% saline with the addition of 0.1% ascorbic acid for apomorphine. NRA0160 is dissolved in a minimal amount of 0.5N HCl and distilled water for injection, then titrated is with 0.5N NaOH to a final pH of 5.

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

NRA-0160 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-0160204718-47-8NRA0160NRA 0160Dopamine Receptor5-HT ReceptorAdrenergic ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorBeta ReceptorInhibitorinhibitorinhibit

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