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 ()
Terazosine ()
Blavin ()
Hytrin ()
Zayasel ()
Fosfomic ()
Flotrin dihydrate ()
Terazosin HCl Dihydrate ()
Dysalfa dihydrate ()
Heitrin dihydrate ()
Terazosin (hydrochloride dihydrate) ()
Terazosin (hydrochloride) ()
Hytrin, Zayasel, Terazosine, Flumarc, Fosfomic, Blavin ()
TERAZOSIN HYDROCHLORIDE DIHYDRATE ()
TERAZOSIN HYDROCHLORIDE ANHYDROUS ()
TERAZOSIN HCL 2H20 ()
BENPH ()
ITRIN ()
ABBOTT-45975 ANHYDROUS ()
HYTRACIN ()
HEITRIN ()
TERAZOSIN (AS HYDROCHLORIDE) ()
HYTRIN BPH ()
NSC-759168 ()
TERAZOSIN HYDROCHLORIDE HYDRATE ()
URODIE ()
Tezruly ()
Terazosabb ()
Terazosina ()
TEZRULY ()
P&D ID
PD002848
CAS
63074-08-8
63590-64-7
141269-45-6
70024-40-7
Tags
available
probe
drug
Approved by
FDA
First approval
1987
Drug indication
Benign prostatic hyperplasia
Drug Status
approved
Max Phase
4.0
Probe info
Probe type
experimental probe
Probe sources
Nature Chemical Biology Probes
Probe targets
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Terazosin hydrochloride is a quinazoline derivative and a competitive and orally active ¦Á1-adrenoceptor antagonist. Terazosin hydrochloride works by relaxing blood vessels and the opening of the bladder. Terazosin hydrochloride has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment[1][2][3].
PRICE 29
DESCRIPTION Terazosin hydrochloride dihydrate is a quinazoline derivative and a competitive and orally active ¦Á1-adrenoceptor antagonist. Terazosin hydrochloride dihydrate works by relaxing blood vessels and the opening of the bladder. Terazosin hydrochloride dihydrate has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment[1][2][3].
DESCRIPTION Terazosin hydrochloride dihydrate (Heitrin dihydrate) is a selective ??1-adrenoceptor antagonist, used for treatment of symptoms of an enlarged prostate (BPH).
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)
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].
PRICE 29
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)
DESCRIPTION Terazosin hydrochloride dihydrate (Heitrin dihydrate) is a selective α1-adrenoceptor antagonist, used for treatment of symptoms of an enlarged prostate (BPH). (TargetMol Bioactive Compound Library)
DESCRIPTION Terazosin is a quinazoline derivative alpha-1-selective adrenergic blocking agent indicated for benign prostatic hyperplasia and hypertension. Terazosin blocks adrenaline's action on alpha-1 adrenergic receptors, causing relaxation of smooth muscle in blood vessels and the prostate. (Enamine Bioactive Compounds)
DESCRIPTION Terazosin hydrochloride (Hytrin) , a selective alpha1-antagonist, can treat the benign prostatic hyperplasia (BPH). It also can lower blood pressure, so it is a drug of choice for patients with prostate enlargement and hypertension. It works on the smooth muscle of the bladder and the blood vessel walls by blocking the function of adrenaline. (TargetMol Bioactive Compound Library)
Cell lines
0
Organisms
3
Compound Sets
39
AdooQ Bioactive Compound Library
A11740
Axon Medchem Screening Library
3512
Cayman Chemical Bioactives
20216
CeMM library of unique drugs (CLOUD)
ChEMBL Approved Drugs
CHEMBL3989562
CHEMBL611
ChEMBL Drugs
CHEMBL3989562
CHEMBL611
Concise Guide to Pharmacology 2017/18
7302
Concise Guide to Pharmacology 2019/20
7302
Concise Guide to Pharmacology 2021/22
7302
Concise Guide to Pharmacology 2023/24
7302
CZ-OPENSCREEN Bioactive Library
DrugBank
DB01162
DrugBank Approved Drugs
DB01162
DrugCentral
3584
DrugCentral Approved Drugs
3584
DrugMAP
DM3JCVS
DrugMAP Approved Drugs
DM3JCVS
DrugMatrix
Enamine Bioactive Compounds
EBC-07365
Enamine BioReference Compounds
EUbOPEN Chemogenomics Library
EUB0000896
Guide to Pharmacology
7302
JUMP-Target 1 Compound Set
5401
Ki Database
Terazosin
LOPAC library
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL611
MedChem Express Bioactive Compound Library
HY-B0371F
HY-B0371A
Nature Chemical Biology Probes
1657
NCATS Inxight Approved Drugs
8L5014XET7
NIH Clinical Collections (NCC)
Novartis Chemogenetic Library (NIBR MoA Box)
NPC Screening Collection
Prestwick Chemical Library
ReFrame library
Selleckchem Bioactive Compound Library
terazosin
terazosin-hydrochloride-hytrin
TargetMol Bioactive Compound Library
T6701
T0197
The Spectrum Collection
Tocris Bioactive Compound Library
1506
Tocriscreen Total
External IDs
85
Properties
(calculated by RDKit )
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
Pathway
Neuronal Signaling
GPCR/G protein
Neuroscience
MOA
Adrenergic Receptor antagonist
Antagonist
PGK1 activator
alpha1-Adrenoceptor Antagonists
Target
Adrenergic receptor alpha-1
Adrenergic Receptor
α-adrenergic receptor
α1-adrenoceptor
a1A antagonist
KCNH7
Primary Target
Adrenergic ?1 Receptors
Member status
member
Therapeutic Class
Anticancer Agents
Recommended Cell Concentration
None
Source data