产品说明书

Guanfacine HCl

Print
Chemical Structure| 29110-48-3 同义名 : 胍法辛盐酸盐 ;Guanfacine (hydrochloride);Guanfacine Hydrochloride;Intuniv;Tenex;Guanfacine
CAS号 : 29110-48-3
货号 : A810155
分子式 : C9H10Cl3N3O
纯度 : 99%
分子量 : 282.554
MDL号 : MFCD00798230
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:
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].
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 - -
实验方案
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

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