CAS 63590-64-7|Fosfomic|Hytracin|Terazosina [INN-Spanish]|Hytrin|Vasomet|Abbott 45975|Blavin|Hytrinex|Trazosin HCl|Flumarc|Terazosin hydrochloride|Itrin|Terazosin|Heitrin|Urodie|Vicard|6,7-dimethoxy...

基本信息

化学结构

分子式

C₁₉H₂₅N₅O₄

分子量

387.4329

精确质量

387.19065431

电荷

InChI

InChI=1S/C19H25N5O4/c1-26-15-10-12-13(11-16(15)27-2)21-19(22-17(12)20)24-7-5-23(6-8-24)18(25)14-4-3-9-28-14/h10-11,14H,3-9H2,1-2H3,(H2,20,21,22)

InChIKey

VCKUSRYTPJJLNI-UHFFFAOYSA-N

Canonic Smiles

COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)C1CCCO1

Isomeric Smiles

O1C(CCC1)C(=O)N1CCN(CC1)c1nc2c(c(n1)N)cc(OC)c(OC)c2

计算属性

JChem

LogD (pH = 7.4)

0.65

LogD (pH = 5.5)

-0.61

Log P

1.18

可自由旋转的化学键

质子供体

质子受体

里宾斯基五规则

true

Acid pKa

7.80

极化表面积

103.04

极化性

41.73

摩尔折射率

105.18

LOG S

-4.22

数据来源

学术数据

产品目录

数据来源

名称和标识

商标名

FosfomicHytracinHytrinVasometBlavinHytrinexFlumarcItrinHeitrinUrodieVicard

别名

Terazosina [INN-Spanish]Abbott 45975Trazosin HClTerazosin hydrochlorideTerazosinTerazosineTerazosine [INN-French]Terazosin HClTerazosinum [INN-Latin]6,7-dimethoxy-2-[4-(oxolane-2-carbonyl)piperazin-1-yl]quinazolin-4-amineterazosinTerazosine1-(4-Amino-6,7-dimethoxy-2-quinazolinyl)-4-((tetrahydro-2-furanyl)carbonyl)piperazineTerazosin

IUPAC标准名

6,7-dimethoxy-2-[4-(oxolane-2-carbonyl)piperazin-1-yl]quinazolin-4-amine

IUPAC传统名

6,7-dimethoxy-2-[4-(oxolane-2-carbonyl)piperazin-1-yl]quinazolin-4-amine terazosin

API名称

Terazosin

国际非专利药品(INN)

terazosinaterazosinumterazosineterazosin

名称和标识

数据登录号

CAS号

63590-64-7

PubChem SID

4650912916096449656464178

PubChem CID

MDL号

DrugBank ID

SureChEMBL数据库

Reactom Database

R-HSA-390641R-HSA-9617370

CHEBI ID

CHEBI:9445

MetaboLights数据库

MTBLS379MTBLS2145MTBLS1642MTBLS2871MTBLS2406MTBLS2878

LINCS数据库

LSM-4997

维基百科标题

Terazosin

CompTox数据库

DTXSID3023639

Drug Central Database

KEGG ID

Beilstein号

KEGG DRUG Database

ACToR数据库

CHEMBL

数据登录号

化合物性质

理化性质

疏水性(logP)

2.182

溶解度

29.7mg/mL

产品相关信息

纯度

95%

化合物性质

分子相关蛋白质

暂无数据

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分子图谱

暂无数据

点击上传数据

描述信息

DrugBank

DB01162

Drug Groups

approved

Description

Terazosin is a selective alpha1-antagonist used for treatment of symptoms of benign prostatic hyperplasia (BPH). It also acts to lower blood pressure, so it is a drug of choice for men with hypertension and prostate enlargement. It works by blocking the action of adrenaline on smooth muscle of the bladder and the blood vessel walls.

Indication

For the treatment of symptomatic BPH and mild to moderate hypertension.

Pharmacology

Terazosin, classified as a quinazoline, is similar to doxazosin and prazosin. As an α-adrenergic blocking agent, terazosin is used to treat hypertension and BPH. Terazosin produces vasodilation and reduces peripheral resistance but in general has only a slight effect on cardiac output. The antihypertensive effect with chronic dosing is not usually accompanied by reflex tachycardia.

Toxicity

LD₅₀=259.3mg/kg (IV in mice)

Affected Organisms

Humans and other mammals

Biotransformation

Hepatic. One of the four metabolites identified (piperazine derivative of terazosin) has antihypertensive activity.

Absorption

Essentially completely absorbed in man (90% bioavailability).

Half Life

12 hours

Protein Binding

90-94%

Elimination

Approximately 10% of an orally administered dose is excreted as parent drug in the urine and approximately 20% is excreted in the feces.

References

• Cushman WC, Ford CE, Cutler JA, Margolis KL, Davis BR, Grimm RH, Black HR, Hamilton BP, Holland J, Nwachuku C, Papademetriou V, Probstfield J, Wright JT Jr, Alderman MH, Weiss RJ, Piller L, Bettencourt J, Walsh SM: Success and predictors of blood pressure control in diverse North American settings: the antihypertensive and lipid-lowering treatment to prevent heart attack trial (ALLHAT). J Clin Hypertens (Greenwich). 2002 Nov-Dec;4(6):393-404. [Pubmed]

External Links

• [Wikipedia]

• [RxList]

• [Drugs.com]

描述信息

参考文献

PubChem文献

数据源提供

参考文献

生物活性

PubChem BioAssay

生物活性