Prazosin hydrochloride is a well-tolerated, CNS-active α1-adrenergic receptor antagonist, primarily used for research into high blood pressure and alcohol use disorders. It potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC50 of 0.15 nM, and also inhibits organic cation transporters OCT-1 and OCT-3 with IC50s of 1.8 and 13 μM, respectively.
- CNS-active α1-adrenergic receptor antagonist
- Potently inhibits norepinephrine (NE)-stimulated 45Ca efflux
- Inhibits organic cation transporters OCT-1 and OCT-3
- Inhibits proliferation, migration, and invasion of U251 and U87 cells, and promotes apoptosis via the PI3K/AKT/mTOR signaling pathway
- Peripheral administration can suppress central α1-adrenergic-mediated hyperexcitability and stress-induced anxiety