General
Preferred name
TERAZOSIN
Synonyms
TERAZOSIN HYDROCHLORIDE ()
(RS)-6,7-dimethoxy-2-[4-(tetrahydrofuran-2-ylcarbonyl)piperazin-1-yl]quinazolin-4-amine ()
Hytrin BPH ()
ABBOTT-45975 ()
Benph ()
Terazosin HCl ()
Hytrin ()
Zayasel ()
Terazosine ()
Fosfomic ()
Blavin ()
Terazosin (hydrochloride dihydrate) ()
Terazosin (hydrochloride) ()
Terazosin HCl Dihydrate ()
Hytrin, Zayasel, Terazosine, Flumarc, Fosfomic, Blavin ()
Terazosin (as hydrochloride) ()
Terazosin hydrochloride dihydrate ()
ABBOTT-45975 ANHYDROUS ()
Urodie ()
Terazosin hydrochloride anhydrous ()
Itrin ()
Terazosin hcl 2h20 ()
NSC-759168 ()
Heitrin ()
TERAZOSIN HYDROCHLORIDE HYDRATE ()
Hytracin ()
Terazosabb ()
P&D ID
PD002848
CAS
63074-08-8
63590-64-7
141269-45-6
70024-40-7
Tags
probe
natural product
drug
available
Approved by
FDA
First approval
1987
Drug Status
approved
Drug indication
Antihypertensive
Benign prostatic hyperplasia
Max Phase
Phase 4
Probe info
Probe type
experimental probe
Probe sources
Probe targets
[[ compound.targets[t].gene_name ]]
Probe control
Probe control not defined
Orthogonal probes
4
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
PHARMACODYNAMICS
Terazosin is a quinazoline derivative alpha-1-selective adrenergic blocker[FDA Label][A176831,A176837].
ABSORPTION
Approximately 90%[A176831].
ROE
Approximately 10% of the oral dose is excreted unchanged in the urine and approximately 20% is excreted in the feces[FDA Label][A176831]. 40% of the total dose is eliminated in urine and 60% of the total dose is eliminated in the feces[FDA Label][A176831].
INDICATION
Terazosin is indicated for use in treating symptomatic benign prostatic hyperplasia and hypertension[FDA Label].
TOXICITY
In the event of an overdose, patients may experience hypotension[FDA Label]. Blood pressure and heart rate should be controlled by having the patient lie down or by treating with volume expanders or if necessary vasopressors[FDA Label]. Patients should be monitored for renal function[FDA Label]. Because terazosin is highly protein bound, dialysis is unlikely to provide benefit to overdosing patients[FDA Label].; ; The oral LD50 in mice is 5500mg/kg[MSDS].
HALF-LIFE
Terazosin has a mean half life 12 hours though this can be as high as 14 hours in patients over 70 years and as low as 11.4 hours in patients 20 to 39 years old[FDA Label][A176831].
METABOLISM
The majority of terazosin is hepatically metabolized[A176831]. The metabolites recovered include 6-O-demethyl terazosin, 7-O-methyl terazosin, a piperozine derivative, and a diamine derivative[A176831].
DESCRIPTION
Postsynaptic α1-adrenoceptor inhibitor.
Marketed formulations may contain terazosin hydrochloride (PubChem CID 44383). (GtoPdb)
Marketed formulations may contain terazosin hydrochloride (PubChem CID 44383). (GtoPdb)
MOA
Terazosin is selective for alpha-1-adrenoceptors but not their individual subtypes[A5212,A5457]. Inhibition of these alpha-1-adrenoceptors results in relaxation of smooth muscle in blood vessels and the prostate, lowering blood pressure and improving urinary flow[A176831,A176837,A5212,A5457]. Smooth muscle cells accounts for roughly 40% of the volume of the prostate and so their relaxation reduces pressure on the urethra[A176837].; ; It has also been shown that catecholamines induce factors responsible for mitogenesis and alpha-1-adrenergic receptor blockers inhibit this effect[A176837].; ; A final long term mechanism of terazosin and other alpha-1-adrenergic receptor blockers is the induction of apoptosis of prostate cells[A176837]. Treatment with terazosin enhances the expression of transforming growth factor beta-1 (TGF-beta1), which upregulates p27kip1, and the caspase cascade[A176837,A176840].
DESCRIPTION
Potent and selective beta3 antagonist
(Tocris Bioactive Compound Library)
DESCRIPTION
α1 and α2B antagonist (α1 > α2B). Orally active
(Tocriscreen Total)
DESCRIPTION
alpha1-Adrenoceptor antagonist
(LOPAC library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
0
Organisms
3
Compound Sets
36
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
Cayman Chemical Bioactives
CeMM library of unique drugs (CLOUD)
ChEMBL Approved Drugs
ChEMBL Drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
DrugMatrix
Enamine BioReference Compounds
Guide to Pharmacology
JUMP-Target 1 Compound Set
Ki Database
LOPAC library
LSP-MoA library (Laboratory of Systems Pharmacology)
Nature Chemical Biology Probes
NCATS Inxight Approved Drugs
NIH Clinical Collections (NCC)
Novartis Chemogenetic Library (NIBR MoA Box)
NPC Screening Collection
Prestwick Chemical Library
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
The Spectrum Collection
Tocris Bioactive Compound Library
Tocriscreen Total
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
82
Molecular Weight
387.19
Hydrogen Bond Acceptors
8
Hydrogen Bond Donors
1
Rotatable Bonds
4
Ring Count
4
Aromatic Ring Count
2
cLogP
1.06
TPSA
103.04
Fraction CSP3
0.53
Chiral centers
1.0
Largest ring
6.0
QED
0.83
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Selectivity
alpha1
Target
Adrenergic Receptor
Adrenergic receptor alpha-1
??-adrenergic receptor
a1A antagonist
KCNH7
Pathway
GPCR/G protein
Neuronal Signaling
MOA
Adrenergic Receptor antagonist
Antagonist
PGK1 activator
alpha1-Adrenoceptor Antagonists
Primary Target
Adrenergic ?1 Receptors
Member status
member
Therapeutic Class
Anticancer Agents
Source data
