Home GPCR & G Protein Adrenergic Receptor antagonist Terazosin HCl For research use only.

Terazosin HCl

Synonyms: Hytrin, Zayasel, Terazosine, Flumarc, Fosfomic, Blavin

Terazosin (Hytrin, Zayasel, Terazosine, Flumarc, Fosfomic, Blavin) is a selective alpha-1 antagonist used for treatment of symptoms of an enlarged prostate (BPH). It works by blocking the action of adrenaline on smooth muscle of the bladder and the blood vessel walls.

Terazosin HCl Chemical Structure

Terazosin HCl Chemical Structure

CAS: 63074-08-8

Selleck's Terazosin HCl has been cited by 1 publication

Purity & Quality Control

Batch: Purity: 99.69%
99.69

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Biological Activity

Description Terazosin (Hytrin, Zayasel, Terazosine, Flumarc, Fosfomic, Blavin) is a selective alpha-1 antagonist used for treatment of symptoms of an enlarged prostate (BPH). It works by blocking the action of adrenaline on smooth muscle of the bladder and the blood vessel walls.
Targets
alpha1-AR [1]
In vitro
In vitro Terazosin induces cytotoxicity in PC-3 and human benign prostatic cells with an IC50 of more than 100 μM. Terazosin also effectively inhibited vascular endothelial growth factor induced proliferation and tube formation in cultured human umbilical vein endothelial cells (IC50 9.9 and 6.8 μM, respectively)[3].
Cell Research Cell lines Human prostate adenocarcinoma PC-3 cells
Concentrations 100 μM
Incubation Time 12 h
Method

To determine the cytotoxic effect mode of action, several identification techniques were used in the current study. Apoptotic cells are detected in situ using terminal deoxynucleotidyl transferase deoxyuridine triphosphate nick end labeling. Results show a positive reaction after a 12-hour treatment of PC-3 cells with terazosin (100 μM).
In Vivo
In vivo Terazosin produces a dose-dependent, complete inhibition of motor activity and catalepsy. Intraventricularly administered this antagonist protects striatal and cerebral cortical alpha 1 receptors but not striatal or cortical D1 receptors from in vivo alkylation by N-ethoxycarbonyl-2-ethoxy-1,2-dihydroxyquinoline. Intraventricular terazosin also produces hypothermia and a reduced respiratory rate suggestive of a reduced sympathetic outflow. Terazosin does not impair performance on a horizontal wire test or the ability to make co-ordinated movements in a swim test[2].Terazosin significantly inhibits vascular endothelial growth factor induced angiogenesis in nude mice with an IC50 of 7.9 μM, showing that it has a more potent anti-angiogenic than cytotoxic effect[3].
Animal Research Animal Models Mice
Dosages 0.05 mg/kg
Administration oral administration
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04760860 Not yet recruiting Dementia With Lewy Bodies Qiang Zhang|University of Iowa October 2024 Phase 1|Phase 2
NCT04551040 Active not recruiting Healthy University of Iowa|Michael J. Fox Foundation for Parkinson''s Research March 26 2021 Phase 1
NCT04386317 Recruiting REM Sleep Behavior Disorder|Pre-motor Parkinson''s Disease|Symptomatic Parkinson Disease Cedars-Sinai Medical Center November 1 2020 Phase 2
NCT00449683 Completed Hyperhidrosis Thomas Jefferson University|National Alliance for Research on Schizophrenia and Depression March 2007 Phase 4
NCT00237510 Completed Antidepressant Induced Excessive Sweating Thomas Jefferson University May 2005 Not Applicable
NCT02244333 Completed Prostatic Hyperplasia Boehringer Ingelheim February 2004 --

Chemical lnformation & Solubility

Molecular Weight 423.89 Formula

C19H25N5O4.HCl
CAS No. 63074-08-8 SDF Download Terazosin HCl SDF
Smiles COC1=C(C=C2C(=C1)C(=NC(=N2)N3CCN(CC3)C(=O)C4CCCO4)N)OC.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 84 mg/mL ( (198.16 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 1 mg/mL

Ethanol : Insoluble


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