产品描述:
Prazosin is an antagonist of α1-adrenergic receptors (α1-ARs).{22637,22636} It selectively binds to α1-ARs with Ki values of 0.2, 0.25, and 0.32 nM for the human recombinant α1A-, α1B-, and α1D-ARs, respectively, over α2-ARs (Kis = 340 and 3.7 nM in α2A-AR-expressing HT-29 cells and α2B-AR-expressing NG108 cells, respectively).{29094,46466} It also binds to melatonin receptor 3 (MT3) in hamster brain membranes (IC50 = 7.8 nM).{22638} Prazosin inhibits peripheral and central postsynaptic α1-ARs with IC50 values of 0.2 and 1.7 nM in isolated dog aorta and rat brain, respectively.{22637} It decreases diastolic blood pressure in normal, renal hypertensive, and spontaneously hypertensive rats when administered at a dose of 1 mg/kg.{46467} Prazosin (1.5 mg/kg) increases the number of entries and percentage of time spent in the open arms of the elevated plus maze, indicating anxiolytic-like activity, in alcohol-consuming rats and also reduces alcohol intake and alcohol-seeking behavior in alcohol-preferring rats.{46468,46469}