Repositioning Candidate Details

Candidate ID: R0152
Source ID: DB00457
Source Type: approved
Compound Type: small molecule
Compound Name: Prazosin
Synonyms: 1-(4-Amino-6,7-dimethoxy-2-quinazolinyl)-4-(2-furanylcarbonyl)piperazine; 2-(4-(2-Furoyl)piperazin-1-yl)-4-amino-6,7-dimethoxyquinazoline; Prazosin
Molecular Formula: C19H21N5O4
SMILES: COC1=C(OC)C=C2C(N)=NC(=NC2=C1)N1CCN(CC1)C(=O)C1=CC=CO1
Structure:
DrugBank Description: Prazosin, also known as _Minipress_, is a drug used to treat hypertension. Prazosin is marketed by _Pfizer_ and was initially approved by the FDA in 1988 . It belongs to the class of drugs known as alpha-1 antagonists , . Recently, many studies have evaluated the benefits of this drug in controlling the symptoms of post-traumatic stress disorder (PTSD) and associated nightmares .
CAS Number: 19216-56-9
Molecular Weight: 383.4011
DrugBank Indication: This drug is indicated for the treatment of hypertension (high blood pressure). Prazosin can be given alone or given with other blood pressure-lowering drugs, including diuretics or beta-adrenergic blocking agents . Prazosin does not negatively impact lung function, and therefore may be used to manage hypertension in patients who are asthmatic or patients with chronic obstructive lung disease (COPD).
DrugBank Pharmacology: **Effects on blood pressure** The pharmacodynamic and therapeutic effect of this drug includes is a decrease in blood pressure as well as clinically significant decreases in cardiac output, heart rate, blood flow to the kidney, and glomerular filtration rate. The decrease in blood pressure may occur in both standing and supine positions . Many of the above effects are due to vasodilation of blood vessels caused by prazosin, resulting in decreased peripheral resistance , . Peripheral resistance refers to the level resistance of the blood vessels to blood that flows through them. As the blood vessels constrict (narrow), the resistance increases and as they dilate (widen), and peripheral resistance decreases, lowering blood pressure . **Effects on sleep disturbance related to post-traumatic stress disorder (PTSD)** Some studies have suggested that this drug improves sleep in patients suffering from insomnia related to nightmares and post-traumatic stress disorder, caused by hyperarousal . This effect likely occurs through the inhibition of adrenergic stimulation found in states of hyperarousal .
DrugBank MoA: Alpha-adrenergic receptors are essential for the regulation of blood pressure in humans. Two types of alpha receptors, alpha 1 and alpha 2, both play a role in regulating blood pressure. Alpha-1 receptors are postsynaptic (located after the nerve junction, or space between a nerve fiber and target tissue). In this case, the target tissue is the vascular smooth muscle . These receptors, when activated, increase blood pressure . Prazosin inhibits the postsynaptic alpha-1 adrenoceptors. This inhibition blocks the vasoconstricting (narrowing) effect of catecholamines (epinephrine and norepinephrine) on the vessels, leading to peripheral blood vessel dilation. Through blood vessel constriction by adrenergic receptor activation, epinephrine and norepinephrine normally act to increase blood pressure .
Targets: Alpha-1A adrenergic receptor antagonist; Alpha-1B adrenergic receptor antagonist; Alpha-1D adrenergic receptor antagonist; Potassium voltage-gated channel subfamily H member 2 inhibitor; Alpha-2A adrenergic receptor binder; Alpha-2B adrenergic receptor binder; Alpha-1 adrenergic receptors
Inclusion Criteria: Indication associated

Strategy ID Strategy Synonyms Related Targets Related Drugs

Target ID Target Name GENE Action Class UniProtKB ID Entry Name

Diseases ID DO ID Disease Name Definition Class
I12 10763 Hypertension An artery disease characterized by chronic elevated blood pressure in the arteries. https://en.wikipedia.org/wiki/Hypertension, https://www.ncbi.nlm.nih.gov/pubmed/24352797 disease of anatomical entity/ cardiovascular system disease/vascular disease/ artery disease Details