2. GPCR/G Protein
  3. Adenosine Receptor
  4. TRR469

TRR469 是一种 A1 腺苷受体 (A1AR) 正性变构调节剂。TRR469 能显著提高 2-chloro N(6)-cyclopentyladenosine (CCPA) 与 A₁AR 的亲和力，增加激动剂放射性配体 [³H]-CCPA 可识别的受体数量。TRR469 在焦虑和疼痛模型中均显示显著效果。TRR469 可用于研究焦虑症和疼痛管理。

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TRR469

TRR469 Chemical Structure

CAS No. : 1394867-58-3

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TRR469 相关抗体

Top Publications Citing Use of Products

查看 Adenosine Receptor 亚型特异性产品:

查看所有亚型
Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TRR469 is a positive allosteric modulator of the A1 adenosine receptor (A1AR). TRR469 significantly increases the affinity of 2-chloro N(6)-cyclopentyladenosine (CCPA) for A₁AR, increasing the number of receptors recognized by the agonist radioligand [³H]-CCPA. TRR469 shows significant effects in both anxiety and pain models. TRR469 can be used to study anxiety disorders and pain management[1][2].

体外研究
(In Vitro)

TRR469 (10 μM) 通过增强小鼠脊髓中 A₁AR 的激活来抑制兴奋性神经递质的释放[1]。

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

TRR469 相关抗体:
体内研究
(In Vivo)

TRR469 (0.01-3 mg/kg，腹腔注射，单次给药) 对小鼠的急性炎症性疼痛、化学性疼痛和机械性异常疼痛具有显著的镇痛作用[1]。
TRR469 (0.3-3 mg/kg，腹腔注射，单次给药) 在所有四种焦虑模型中均表现出剂量依赖性的抗焦虑作用[2]。

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

Animal Model: Formalin test, writhing test, and diabetic neuropathic pain model established in CD-1 mice[1]
Dosage: 0.01, 0.03, 1 and 3 mg/kg
Administration: Intraperitoneal injection (i.p.), single dose
Result: Showed dose-dependent analgesic effect with ED50s of 0.257 and 0.171 mg/kg in formalin test and writhing test.
Dose-dependent reversaled mechanical abnormal pain.
Animal Model: Elevated cross maze test, the light-dark box test, the opening test and the buried pearl test established in CD-1 mice[2]
Dosage: 0.3, 1 and 3 mg/kg
Administration: Intraperitoneal injection (i.p.), single dose
Result: Demonstrated dose-dependent anti-anxiety effects in all four anxiety models.
Did not enhance the sedative effect of ethanol, nor does it impair the motor coordination function.
分子量

506.03

Formula

C28H25ClFN3OS
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

TRR469 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:

TRR4691394867-58-3TRR 469TRR-469Adenosine ReceptorP1 receptorA1 adenosine receptorsPositive allosteric modulatorTRR469 AnalgesiaAcute and chronic painInhibitorinhibitorinhibit

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目录号：
HY-112567
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