基本信息

技术规格

物性(参考值)

安全信息

图形或危害标志
信号词	危险
危险性说明	H301 : 吞咽会中毒。
防范说明	P501 : 将内装物/容器送到批准的废物处理厂处理。 P270 : 使用本产品时不要进食、饮水或吸烟。 P264 : 作业后彻底清洗皮肤。 P301 + P310 + P330 : 如误吞咽：立即呼叫急救中心/医生。漱口。 P405 : 存放处须加锁。

相关法规

运输信息

基本信息

产品描述

Guanfacine Hydrochloride是一种选择性的α2A-肾上腺素受体激动剂，具有降压效果。

靶点（IC50 & Targe）

α2A-adrenoceptor

细胞实验

Cell lines: LLC-PK1和LLC-PK1/MDR1细胞

Concentrations: 5 μM

Incubation Time: 1 h

Method:1 mL细胞以一定密度被接种于24孔板中。每两天更换一次培养基，直到细胞到达融合。为了研究P-gp对guanfacine运输的潜在影响，在LLC-PK1/MDR1细胞和P-gp-negative LLC-PK1细胞中对胞内guanfacine的积累进行测定。罗丹明6G（Rhodamine6G），一种众所周知的P-gp底物，用于作为阳性对照。细胞融合后，将transport buffer替换原来的培养基，在37℃孵育30分钟。30分钟后，移去transport buffer，加入所检测的化合物（5 μM rhodamine6G, 5 μM guanfacine, or 50 μM guanfacine），继续孵育60分钟。然后将溶液倒掉，用预冷的Dulbecco’s phosphate-buffered saline（含1% Triton X-100）对细胞进行洗涤，洗涤3次。在530 nm激发波长和580 nm发射波长下检测胞内罗丹明6G的积累，使用高效液相色谱分析法分析细胞内残留的guanfacine。

(Only for Reference)

动物实验

Animal Models: 大鼠

Formulation: 生理盐水

Dosages: 0.075, 0.15, 0.3和0.6 mg/kg

Administration: 腹腔注射

(Only for Reference)

参考文献

[1] Sagvolden T, et al. Behav Brain Funct. 2006, 2:41.

[2] Gillis NK, et al. Neuropsychiatr Dis Treat. 2011, 7:501-5.

安全信息

图形或危害标志
危险说明	H302 H410
防范说明	P264 P270 P273 P301+P312 P330 P391 P501
UN号码	3077
危险分类	9
包装等级	III
WGK	3

产品说明

应用

Guanfacine hydrochloride has been used as an α2A adrenoceptor agonist to test its protective effect on hypobaric hypoxia (HH) and in rat brain to measure blood oxygenation level dependent (BOLD) response.

生化/生理作用

Guanfacine stimulates the brain postsynaptic α2 adrenergic receptor (AR) and mediates the prefrontal cortical (PFC) neuronal regulation and strengthens their network. Guanfacine improves the density of neuronal dendrites and is useful in treating neuropsychiatric disorders. It modulates the synaptic and cytoskeletal proteins expression in prefrontal cortical (PFC) neurons and may improve hypobaric hypoxia (HH) induced PFC dysfunctions. Guanfacine enhances cognitive function and is recommended for attention deficit hyperactivity disorder (ADHD) therapy.
α-2 noradrenergic receptor agonist.

特点和优势

This compound was developed by Promius. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

基本信息

产品性质

安全信息

产品说明

一般描述

Guanfacine hydrochloride, is a selective α-adrenergic receptor agonist, that is used in the treatment of attention deficit hyperactivity disorder (ADHD) and hypertension.
Pharmaceutical secondary standards for application in quality control, provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards.

应用

Guanfacine hydrochloride may be used as a pharmaceutical reference standard for the determination of the analyte in bulk drug and pharmaceutical formulations by spectrophotometry and high performance liquid chromatography.
These Secondary Standards are qualified as Certified Reference Materials. These are suitable for use in several analytical applications including but not limited to pharma release testing, pharma method development for qualitative and quantitative analyses, food and beverage quality control testing, and other calibration requirements.

生化/生理作用

α-2 noradrenergic receptor agonist.

分析说明

These secondary standards offer multi-traceability to the USP, EP and BP primary standards, where they are available.

其他说明

This Certified Reference Material (CRM) is produced and certified in accordance with ISO 17034 and ISO/IEC 17025. All information regarding the use of this CRM can be found on the certificate of analysis.

附注

To see an example of a Certificate of Analysis for this material enter LRAC3708 in the Documents slot below. This is an example certificate only and may not be the lot that you receive.

基本信息

产品性质

安全信息

产品说明

一般描述

This product is provided as delivered and specified by the issuing Pharmacopoeia. All information provided in support of this product, including SDS and any product information leaflets have been developed and issued under the Authority of the issuing Pharmacopoeia.
For further information and support please go to the website of the issuing Pharmacopoeia.

生化/生理作用

α-2 noradrenergic receptor agonist.

分析说明

These products are for test and assay use only. They are not meant for administration to humans or animals and cannot be used to diagnose, treat, or cure diseases of any kind.  ​

其他说明

Sales restrictions may apply.

基本信息

产品性质

安全信息

基本信息