| 产品描述： | Guanfacine (hydrochloride) is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) |
| 靶点： |
Adrenergic Receptor;AdrenergicReceptor |
| 体外研究： |
Guanfacine (hydrochloride) increases the delay-related neuronal firing needed for working memory on dIPFC neurons at the cellular level. Guanfacine improves PFC cognitive function by inhibiting the production of CAMP, closing HCN channels, and strengthening the PFC networks |
| 体内研究： |
Guanfacine (hydrochloride) enhances PFC working memory function in aged monkeys and improves impulse control in monkeys performing a delayed discounting task. Guanfacine improves cognitive performance when infused directly into the rat or monkey PFC. Guanfacine blocks 2A receptors in the monkey dIPFC markedly impairs working memory, behavioral inhibition and greatly reduces persistent neuronal firing |
| 细胞实验： |
Cells (1 mL) are seeded into 24-well plates at a density of 1 × 105 cells/mL. Culture medium is replaced every two days until cells reached confluence. To investigate the potential influence of P-gp on guanfacine transport, intracellular accumulation of guanfacine is measured in LLC-PK1/MDR1 cells and P-gp-negative LLC-PK1 cells. Rhodamine6G, a well-known P-gp substrate, is included as a positive control. After cells reach confluence, the culture medium is replaced by transport buffer for a 30-minute preincubation at 37°C. Transport buffer is then removed and the test compounds (5 μM rhodamine6G, 5 μM guanfacine, or 50 μM guanfacine) are added, and an additional 60-minute incubation period commenced. Next, the solutions are discarded, and the cells are washed three times with ice-cold Dulbecco’s phosphate-buffered saline and solubilized with 1% Triton X-100. Intracellular accumulation of rhodamine6G is measured using a fluorescent microplate reader with a 530 nm excitation and a 580 nm emission wavelength, wh |
| 参考文献： |
1. Amy F T Arnsten, et al. Guanfacine for the treatment of cognitive disorders: a century of discoveries at Yale. Yale J Biol Med. 2012 Mar;85(1):45-58. Epub 2012 Mar 29. 2. P. A. Van Zwieten, et al. The pharmacology of centrally acting antihypertensive drugs. Br J Clin Pharmacol. 1983; 15(Suppl 4): 455S–462S. 3. Min Wang, et al. Alpha2A-adrenoceptors strengthen working memory networks by inhibiting cAMP-HCN channel signaling in prefrontal cortex. Cell. 2007 Apr 20;129(2):397-410. |
| 溶解性： |
Soluble in DMSO、H2O |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.539 ml |
17.696 ml |
35.392 ml |
| 5 mM |
0.708 ml |
3.539 ml |
7.078 ml |
| 10 mM |
0.354 ml |
1.77 ml |
3.539 ml |
| 50 mM |
0.071 ml |
0.354 ml |
0.708 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京