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/ Guanfacine HCl

盐酸胍法辛 /Guanfacine HCl {[allProObj[0].p_purity_real_show]}

货号：A810155 同义名： 胍法辛盐酸盐 / Guanfacine (hydrochloride);Guanfacine Hydrochloride Ambeed 开学季，买赠积分，赢豪礼

Guanfacine HCl is a centrally acting antihypertensive with α2-adrenoceptor agonist with Kd value of 31 nM for α2A-adrenoceptor while displaying 60-fold selectivity over α2B-adrenoceptors, causing a decrease in heart rate and peripheral vascular resistance.

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Guanfacine HCl 化学结构 CAS号：29110-48-3
Guanfacine HCl 化学结构
CAS号：29110-48-3
Guanfacine HCl 3D分子结构
CAS号：29110-48-3
Guanfacine HCl 化学结构 CAS号：29110-48-3
Guanfacine HCl 3D分子结构 CAS号：29110-48-3
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Guanfacine HCl 纯度/质量文件 产品仅供科研

货号：A810155 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Adrenergic Receptor ↓ α-adrenergic receptor ↓ β-adrenergic receptor ↓ 其他靶点 纯度
Ivabradine HCl ✔ {[allProObj[0].p_purity_real_show]}
Maprotiline hydrochloride ✔ {[allProObj[0].p_purity_real_show]}
Cisatracurium besylate ✔ {[allProObj[0].p_purity_real_show]}
Yohimbine HCI ✔ {[allProObj[0].p_purity_real_show]}
BMY 7378 ++

α1D-adrenoceptor, pKi: 5.1

α2C-adrenoceptor, pKi: 6.54

 		+

β1-adrenoceptor, pIC50: 5.1

 		{[allProObj[0].p_purity_real_show]}
Asenapine maleate ++++

α2A-adrenergic receptor, pKi: 8.9

α2B-adrenergic receptor, pKi: 8.9

 		{[allProObj[0].p_purity_real_show]}
Piribedil ++

adrenoceptor α2A, pKi: 7.1

adrenoceptor α2C, pKi: 7.2

 		{[allProObj[0].p_purity_real_show]}
Prazosin HCl ✔ {[allProObj[0].p_purity_real_show]}
Silodosin ✔ {[allProObj[0].p_purity_real_show]}
Phenoxybenzamine HCl ✔ {[allProObj[0].p_purity_real_show]}
Naftopidil +++

α1A-adrenergic receptor, Ki: 3.7 nM

α1D-adrenergic receptor, Ki: 20 nM

 		{[allProObj[0].p_purity_real_show]}
Naftopidil 2HCl +

α1-adrenergic receptor, IC50: 0.2 μM

 		{[allProObj[0].p_purity_real_show]}
Alfuzosin HCl ✔ {[allProObj[0].p_purity_real_show]}
Terazosin HCl ✔ {[allProObj[0].p_purity_real_show]}
Atipamezole ✔ {[allProObj[0].p_purity_real_show]}
Phentolamine methanesulfonate salt ✔ {[allProObj[0].p_purity_real_show]}
Doxazosin mesylate ✔ {[allProObj[0].p_purity_real_show]}
Tolazoline HCl ✔ {[allProObj[0].p_purity_real_show]}
Zenidolol hydrochloride ++++

β1-adrenergic receptor, Ki: 611nM

β2-adrenergic receptor, Ki: 0.7nM

 		{[allProObj[0].p_purity_real_show]}
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Guanfacine HCl 生物活性

描述 Guanfacine hydrochloride, an anti-hypertensive agent. Extended-release guanfacine appears to be safe and effective for reducing hyperactivity, impulsiveness, and distractibility in children with ASD (autism spectrum disorder)[3]. Guanfacine lowers blood pressure by activating CNS alpha adrenoreceptors, which results in sympathetic outflow leading to reduced vascular tone. Guanfacine is rapidly and completely absorbed from the gastrointestinal tract and apparently undergoes extensive distribution to all tissues. Guanfacine's adverse reactions include dry mouth, sedation, and constipation. Adverse effects and reaction to sudden withdrawal of the drug may be less severe with guanfacine than with clonidine[4]. Guanfacine extended release (ER), as a new option to the treatment of attention deficit hyperactivity disorder, which acts at postsynaptic level. Guanfacine stimulates postsynaptic alfa-2A adrenergic receptors so it inhibits the production of cAMP and closes HCN channels enhancing the effectiveness of the signal of the pyramidal neurons of the prefrontal cortex, thus improving working memory and attention[5].

Guanfacine HCl 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02204410 Attention Deficit Hyperactivit... 展开 >>y Disorder Deficient Emotional Self-Regulation 收起 << Phase 4 Completed - United States, Massachusetts ... 展开 >> Massachusetts General Hospital Boston, Massachusetts, United States, 02114 收起 <<
NCT01172288 Tourettes Syndrome ... 展开 >> Tic 收起 << Phase 2 Completed - United States, Connecticut ... 展开 >> Yale Child Study Center New Haven, Connecticut, United States, 06520 收起 <<
NCT00684489 Hypertension Not Applicable Completed - -

Guanfacine HCl 参考文献

[1]Gillis NK, Zhu HJ, et al. An in vitro evaluation of guanfacine as a substrate for P-glycoprotein. Neuropsychiatr Dis Treat. 2011;7:501-5.

[2]Sagvolden T. The alpha-2A adrenoceptor agonist guanfacine improves sustained attention and reduces overactivity and impulsiveness in an animal model of Attention-Deficit/Hyperactivity Disorder (ADHD). Behav Brain Funct. 2006 Dec 15;2:41.

[3]Board AW, Perry VP, Shepperson BE, Nyman CE, Carchman SH. A postmarketing evaluation of guanfacine hydrochloride in mild to moderate hypertension. Clin Ther. 1988;10(6):761-775

[4]Cornish LA. Guanfacine hydrochloride: a centrally acting antihypertensive agent. Clin Pharm. 1988;7(3):187-197

[5]Alamo C, López-Muñoz F, Sánchez-García J. Mechanism of action of guanfacine: a postsynaptic differential approach to the treatment of attention deficit hyperactivity disorder (adhd). Actas Esp Psiquiatr. 2016;44(3):107-112

Guanfacine HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.54mL

0.71mL

0.35mL

17.70mL

3.54mL

1.77mL

35.39mL

7.08mL

3.54mL

Guanfacine HCl 技术信息

CAS号29110-48-3
分子式C9H10Cl3N3O
分子量 282.554
别名 胍法辛盐酸盐 ;Guanfacine (hydrochloride);Guanfacine Hydrochloride;Intuniv;Tenex;Guanfacine
运输蓝冰
存储条件

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度

DMSO: 30 mg/mL(106.17 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 20 mg/mL(70.78 mM)，配合低频超声助溶
动物实验配方

Tags: Guanfacine | 29110-48-3 | α2A Agonist | GPCR/G Protein | Neuronal Signaling | Adrenergic Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Guanfacine HCl 纯度/质量文件 | Guanfacine HCl 亚型比较 | Guanfacine HCl 生物活性 | Guanfacine HCl 临床数据 | Guanfacine HCl 参考文献 | Guanfacine HCl 实验方案 | Guanfacine HCl 技术信息

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