Share this post on:

product name Terazosin HCl


Description: Terazosin HCl is a selective α1-adrenoceptor antagonist, used for treatment of symptoms of an enlarged prostate (BPH). 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).

References: Neuroscience. 1999;94(4):1245-52; J Urol. 2003 Feb;169(2):724-9.



Molecular Weight (MW)

459.92 
Formula

C19H25N5O4.HCl.2H2
CAS No.

70024-40-7 
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: > 10 mM
Water
Ethanol
Solubility (In vivo)

 
Synonyms

 

other peoduct :References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/19398705

In Vitro

In vitro activity: 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)


Kinase Assay:


Cell Assay: 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 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 coordinated movements in a swim test. 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. 
Animal model Mice 
Formulation & Dosage Dissolved in water; 0.05 mg/kg; oral gavage 
References Neuroscience. 1999;94(4):1245-52; J Urol. 2003 Feb;169(2):724-9. 

Dinoprost (tromethamine salt)

Share this post on:

Author: Sodium channel

Share this post on:

product name Terazosin HCl


Description: Terazosin HCl is a selective α1-adrenoceptor antagonist, used for treatment of symptoms of an enlarged prostate (BPH). 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).

References: Neuroscience. 1999;94(4):1245-52; J Urol. 2003 Feb;169(2):724-9.



Molecular Weight (MW)

459.92 
Formula

C19H25N5O4.HCl.2H2
CAS No.

70024-40-7 
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: > 10 mM
Water
Ethanol
Solubility (In vivo)

 
Synonyms

 

other peoduct :References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/19398705

In Vitro

In vitro activity: 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)


Kinase Assay:


Cell Assay: 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 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 coordinated movements in a swim test. 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. 
Animal model Mice 
Formulation & Dosage Dissolved in water; 0.05 mg/kg; oral gavage 
References Neuroscience. 1999;94(4):1245-52; J Urol. 2003 Feb;169(2):724-9. 

Dinoprost (tromethamine salt)

Share this post on:

Author: Sodium channel