Bioactivity | Prazosin hydrochloride is a well-tolerated, CNS-active α1-adrenergic receptor antagonist for the research of high blood pressure and alcohol use disorders[1]. Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC50 of 0.15 nM[2].Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC50s of 1.8, and 13 μM, respectively[3]. |
Invitro | Prazosin (0, 2.5, 5, 7.5, 10, 15, 20, 30, 40 and 50 µM) effectively inhibits the proliferation of U251 and U87 cells[4].Prazosin inhibits the migration and invasion of U251 and U87 cells[4].Prazosin treatment decreases the protein expression of components of the PI3K/AKT/mTOR signaling pathway. Prazosin (13.16 and 11.57 µM for U251 and U87 cells, 48 hours) decreases the expression levels of P70 and cyclin D1, which are downstream target genes of the PI3K/AKT/mTOR signaling pathway[4]. Cell Proliferation Assay Cell Line: |
In Vivo | Peripheral administration of Prazosin (0, 0.5, 1.0, 1.5 or 2.0 mg/kg; i.p.) can suppress not only central α1-adrenergic-mediated hyperexcitability but also stress-induced anxiety[1]. Animal Model: |
Name | Prazosin hydrochloride |
CAS | 19237-84-4 |
Formula | C19H22ClN5O4 |
Molar Mass | 419.86 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
Reference | [1]. Dennis D Rasmussen, et al. The alpha1-adrenergic receptor antagonist, prazosin, reduces alcohol drinking in alcohol-preferring (P) rats. Alcohol Clin Exp Res. 2009 Feb;33(2):264-72. [2]. W S Colucci, et al. Nonlinear relationship between alpha 1-adrenergic receptor occupancy and norepinephrine-stimulated calcium flux in cultured vascular smooth muscle cells.Mol Pharmacol. 1985 May;27(5):517-24. [3]. Deborah L White, et al. OCT-1-mediated influx is a key determinant of the intracellular uptake of imatinib but not nilotinib (AMN107): reduced OCT-1 activity is the cause of low in vitro sensitivity to imatinib.Blood. 2006 Jul 15;108(2):697-704. [4]. Jing Zhang, et al. Prazosin inhibits the proliferation, migration and invasion, but promotes the apoptosis of U251 and U87 cells via the PI3K/AKT/mTOR signaling pathway. Exp Ther Med. 2020 Aug;20(2):1145-1152. |