| Name | Guanfacine hydrochloride |
| Description | Guanfacine hydrochloride (Intuniv) is a centrally acting antihypertensive agent with specificity towards ADRENERGIC ALPHA-2 RECEPTORS. |
| Cell Research | 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. Rhodamine6 g, 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 rhodamine6 g, 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 rhodamine6 g is measured using a fluorescent microplate reader with a 530 nm excitation and a 580 nm emission wavelength, which is a well established method. Cellular retention of guanfacine is analyzed by the high-performance liquid chromatographic assay described below. The concentrations of rhodamine6 g and guanfacine are calculated from their respective standard curves, and standardized with the cellular protein content determined by a Pierce bicinchoninic acid protein kit.(Only for Reference) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 55 mg/mL (194.66 mM), Sonication is recommended.
H2O : 28.3 mg/mL (100 mM)
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| Keywords | hypotension | Inhibitor | inhibit | noradrenergic α2A | tourette's syndrome | sedation | attention deficit hyperactivity disorder (ADHD) | Guanfacine Hydrochloride | α2A receptor | Guanfacine hydrochloride | Adrenergic Receptor | cognitive disorders | prefrontal cortex (PFC) | Beta Receptor |
| Inhibitors Related | Octopamine hydrochloride | Trazodone hydrochloride | Mianserin hydrochloride |
| Related Compound Libraries | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Drug Repurposing Compound Library | Anti-Cancer Approved Drug Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |
United States
