63590-64-7

63590-64-7 structure
63590-64-7 structure
  • Name: Terazosin
  • Chemical Name: terazosin
  • CAS Number: 63590-64-7
  • Molecular Formula: C19H25N5O4
  • Molecular Weight: 387.43300
  • Catalog: API Circulatory system medication Antihypertensive drug
  • Create Date: 2018-08-29 08:00:37
  • Modify Date: 2024-01-02 13:01:09
  • Terazosin is a selective alpha1-antagonist used for treatment of symptoms of benign prostatic hyperplasia (BPH).Target: Alpha-1 Adrenergic ReceptorTerazosin is selective for alpha 1A-adrenoceptors which appear to dominate in the human prostate; the therapeutic relevance of this selectivity remains to be assessed in clinical studies [1]. Administration of terazosin 1 mg orally for 28 d. Terazosin initially shifted the dose-response curve of phenylephrine to the right, with a significant increase in ED50 for phenylephrine from a control value of 102 to 759 ng/min on day 1 of terazosin (P < 0.001). The mean Kd of terazosin was estimated as 11 +/- 15 nM in the first few days of treatment. This study demonstrates that pharmacological tolerance to the alpha 1-adrenoceptor blocking action of terazosin occurs in man and may be responsible for loss in efficacy with chronic therapy [2].

Name terazosin
Synonyms Terazosin Hydrochloride
[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-(oxolan-2-yl)methanone
MFCD00467965
Description Terazosin is a selective alpha1-antagonist used for treatment of symptoms of benign prostatic hyperplasia (BPH).Target: Alpha-1 Adrenergic ReceptorTerazosin is selective for alpha 1A-adrenoceptors which appear to dominate in the human prostate; the therapeutic relevance of this selectivity remains to be assessed in clinical studies [1]. Administration of terazosin 1 mg orally for 28 d. Terazosin initially shifted the dose-response curve of phenylephrine to the right, with a significant increase in ED50 for phenylephrine from a control value of 102 to 759 ng/min on day 1 of terazosin (P < 0.001). The mean Kd of terazosin was estimated as 11 +/- 15 nM in the first few days of treatment. This study demonstrates that pharmacological tolerance to the alpha 1-adrenoceptor blocking action of terazosin occurs in man and may be responsible for loss in efficacy with chronic therapy [2].
Related Catalog
References

[1]. Michel, M.C., et al., Drugs for treatment of benign prostatic hyperplasia: affinity comparison at cloned alpha 1-adrenoceptor subtypes and in human prostate. J Auton Pharmacol, 1996. 16(1): p. 21-8.

[2]. Vincent, J., et al., Pharmacological tolerance to alpha 1-adrenergic receptor antagonism mediated by terazosin in humans. J Clin Invest, 1992. 90(5): p. 1763-8.

Density 1.332 g/cm3
Boiling Point 664.5ºC at 760 mmHg
Melting Point 281-283°C
Molecular Formula C19H25N5O4
Molecular Weight 387.43300
Flash Point 355.7ºC
Exact Mass 387.19100
PSA 103.04000
LogP 1.64090
Storage condition -20°C Freezer
Water Solubility H2O: 25 mg/mL

CHEMICAL IDENTIFICATION

RTECS NUMBER :
TK8044925
CHEMICAL NAME :
Piperazine, 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-((tetrahyd ro-2-furanyl)carbonyl )-
CAS REGISTRY NUMBER :
63590-64-7
LAST UPDATED :
199806
DATA ITEMS CITED :
1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
3 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4734418
Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302
Personal Protective Equipment dust mask type N95 (US);Eyeshields;Gloves
Hazard Codes Xn: Harmful;
Risk Phrases R22
Safety Phrases S26
RIDADR NONH for all modes of transport
WGK Germany 3
RTECS TK8044925

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Literature: US2007/161791 A1, ; Page/Page column 2; 3-4 ;

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Literature: US6313293 B1, ;

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Literature: Synthetic Communications, , vol. 34, # 10 p. 1881 - 1884
Precursor  3

DownStream  0