2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor
  4. AGN-201781

AGN-201781 (compound 11) 是一种具有口服活性的 α-2B 肾上腺素能受体激动剂。AGN-201781 可用于神经性疼痛的相关研究。

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AGN-201781

AGN-201781 Chemical Structure

CAS No. : 628730-30-3

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AGN-201781 相关抗体

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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

AGN-201781 (compound 11) is an orally active α-2B adrenergic receptor agonist. AGN-201781 can be used in studies related to neuropathic pain[1].

体外研究
(In Vitro)

AGN-201781 (compound 11) 是一种强效的、偏好作用于 α-2B 的肾上腺素能激动剂，在 α-2A 受体上无可检测的活性，在 α-2C 受体上活性较弱，在 α-1A 受体上活性极低，在 α-1B 或 α-1D 受体上无活性[1]。

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

AGN-201781 相关抗体:
体内研究
(In Vivo)

AGN-201781 (化合物 11) (灌胃；单剂量，30-1000 μg/kg；皮下渗透泵；持续给药，0.1 mg/kg/hour，5 天) 在 100 μg/kg 及以上的灌胃剂量下可显著缓解急性神经性疼痛[1]。
AGN-201781 (compound 11)(1 mg/kg；腹腔注射；单次给药；0.5 mg/kg；静脉注射；单次给药；3 mg/kg；口服；单次给药) 在高于达到峰值神经性疼痛缓解所需的剂量下，未产生显著的镇静或心血管副作用[1]。

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

Animal Model: Sprague-Dawley (male, 100-120 grams for acute dosing; neuropathic pain Chung model via partial ligation of left spinal nerves L-5 and L-6)[1]
Dosage: 30-1000 μg/kg (acute oral); 0.1 mg/kg/hour (extended subcutaneous)
Administration: p.o.; single dose (acute); subcutaneous osmotic minipump; continuous; 5 days (extended)
Result: Produced no significant allodynia reversal at 30 μg/kg.
Produced 60-90% peak allodynia reversal at 100 μg/kg and 300 μg/kg, with effects diminishing by 140 minutes post-dose.
Produced lower peak allodynia reversal at 1000 μg/kg, with effects diminishing over time.
Achieved ~80% allodynia reversal during 5-day continuous dosing, with analgesic effect maintained at the same level for 30 days post-dosing.
分子量

180.27

Formula

C9H12N2S
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

AGN-201781 相关分类

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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:

AGN-201781628730-30-3AGN201781AGN 201781Adrenergic ReceptorBeta Receptorneuropathic painpost-operative painα-2B adrenergic receptorinflammatory painperipheral analgesiacancer-related painvisceral painbrimonidineα-2C adrenergic receptorsα-2A adrenergic receptorsInhibitorinhibitorinhibit

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