An α1-AR antagonist; selectively binds to α1-ARs (Kis = 0.2

Prazosin (hydrochloride) – 50 mg

Brand:
Cayman
CAS:
19237-84-4
Storage:
-20
UN-No:
Non-Hazardous - /

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}  

 

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Description

An α1-AR antagonist; selectively binds to α1-ARs (Kis = 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); binds to MT3 in hamster brain membranes (IC50 = 7.8 nM); inhibits peripheral and central postsynaptic α1-ARs (IC50s = 0.2 and 1.7 nM in isolated dog aorta and rat brain, respectively); decreases diastolic blood pressure in normal, renal hypertensive, and spontaneously hypertensive rats at 1 mg/kg; increases the number of entries and percentage of time spent in the open arms of the elevated plus maze in alcohol-consuming rats and also reduces alcohol intake and alcohol-seeking behavior in alcohol-preferring rats at 1.5 mg/kg

Formal name: [4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-1-piperazinyl]-2-furanyl-methanone, monohydrochloride

Synonyms:  CP 12,299-1|NSC 292810

Molecular weight: 419.9

CAS: 19237-84-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Kidney & Renal Disease||Research Area|Neuroscience|Behavioral Neuroscience|Addiction Research||Research Area|Neuroscience|Behavioral Neuroscience|Anxiety

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