1. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel Protein Tyrosine Kinase/RTK
  2. mGluR Calcium Channel Trk Receptor
  3. AZD-2066 hydrochloride

AZD-2066 hydrochloride 是一种选择性的,具有口服活性和可透过血脑屏障的 mGluR5 拮抗剂。AZD 2066 hydrochloride 激活 BDNF/trkB 信号通路。AZD 2066 hydrochloride 可用于神经性疼痛、重度抑郁症和胃食管反流病研究。

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AZD-2066 hydrochloride Chemical Structure

AZD-2066 hydrochloride Chemical Structure

CAS No. : 934338-70-2

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AZD-2066 hydrochloride 的其他形式现货产品:

Other Forms of AZD-2066 hydrochloride:

MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AZD-2066 hydrochloride is a selective, orally active and blood-brain barrier-permeating mGluR5 antagonist. AZD 2066 hydrochloride activates the BDNF/trkB signaling pathway. AZD 2066 hydrochloride can be used in the research of neuropathic pain, major depressive disorder and gastroesophageal reflux disease[1][2][3][5].

IC50 & Target[1][2][3][5]

mGluR5

 

体外研究
(In Vitro)

AZD 2066 (1-10 μM) hydrochloride 可抑制 Ca2+ 反应,在 mGlu5/HEK 细胞以及纹状体、海马和皮质培养物中的 IC50 分别为 27.2、3.56、96.2 和 380 nM[4]
AZD 2066 (1-10 μM) hydrochloride 可抑制 DHPG (HY-12598A) 浸浴诱导的 Ca2+ 振荡响应,并阻断 DHPG 或 Quis 在 mGlu5/HEK 细胞中的作用[4]

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

体内研究
(In Vivo)

AZD 2066 (0.3-30 mg/kg,口服,60 min) hydrochloride 在大鼠中有辨别效应[2]
AZD-2066 (10 µM,脑切片灌注) hydrochloride 通过 BDNF/trkB 信号通路减轻慢性社会挫败应激 (CSDS) 处理小鼠中 dihydroxyphenylglycine (DHPG) 促进的长期抑郁 (LTD)[5]
AZD-2066 (5 mg/kg,腹腔注射,2 × 12 h) hydrochloride 可减轻小鼠中慢性社会挫败应激 (CSDS) 诱发的抑郁行为[5]

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

Animal Model: Male Wistar rats (weighing 240-250 g)[2]
Dosage: 0.03, 0.1, 0.3, 1, 3, 10, 30 mg/kg
Administration: Oral gavage (p.o.)
Result: Caused full and dose-dependent AZD9272-appropriate responding.
Animal Model: Depressive model (C57BL/6 mice were subjected to physical defeats that were generated by a CD-1 aggressor for 5 min every day for 10 days)[5]
Dosage: 5 mg/kg
Administration: Intraperitoneal injection (i.p.), 2 × 12 h
Result: Increased social interaction ratio.
Reversed time spent in interaction zone.
Increased sucrose preference scores.
分子量

418.28

Formula

C19H17Cl2N5O2

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
  • 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.

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AZD-2066 hydrochloride
目录号:
HY-110255B
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