Benzthiazide

Các tên gọi khác (11 ) :

3-((Benzylthio)methyl)-6-chloro-7-sulfamoyl-2H-benzo-1,2,4-thiadiazine 1,1-dioxide
3-Benzylthiomethyl-6-chloro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide
3-Benzylthiomethyl-6-chloro-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide
6-chloro-1,1-dioxo-3-(Phenylmethylsulfanylmethyl)-4H-benzo[e][1,2,4]thiadiazine-7-sulfonamide
6-chloro-7-Sulfamoyl-3-benzylthiomethyl-2H-1,2,4-benzothiadiazine 1,1-dioxide
Benzothiazide
Benzotiazida
Benzthiazid
Benzthiazide
Benzthiazidum
Benztiazide

stimulants

Thuốc Gốc

Small Molecule

CAS: 91-33-8

CTHH: C₁₅H₁₄ClN₃O₄S₃

PTK: 431.937

Benzthiazide is used to treat hypertension and edema. Like other thiazides, benzthiazide promotes water loss from the body (diuretics). They inhibit Na+/Cl- reabsorption from the distal convoluted tubules in the kidneys. Thiazides also cause loss of potassium and an increase in serum uric acid. Thiazides are often used to treat hypertension, but their hypotensive effects are not necessarily due to their diuretic activity. Thiazides have been shown to prevent hypertension-related morbidity and mortality although the mechanism is not fully understood. Thiazides cause vasodilation by activating calcium-activated potassium channels (large conductance) in vascular smooth muscles and inhibiting various carbonic anhydrases in vascular tissue.

Nhận Dạng Quốc Tế & Đặc Tính Hóa Học

Công thức hóa học

C₁₅H₁₄ClN₃O₄S₃

Phân tử khối

431.937

Monoisotopic mass

430.983495728

InChI

InChI=1S/C15H14ClN3O4S3/c16-11-6-12-14(7-13(11)25(17,20)21)26(22,23)19-15(18-12)9-24-8-10-4-2-1-3-5-10/h1-7H,8-9H2,(H,18,19)(H2,17,20,21)

InChI Key

InChIKey=NDTSRXAMMQDVSW-UHFFFAOYSA-N

IUPAC Name

3-[(benzylsulfanyl)methyl]-6-chloro-1,1-dioxo-4H-1$l^{6},2,4-benzothiadiazine-7-sulfonamide

Traditional IUPAC Name

benzthiazide

SMILES

NS(=O)(=O)C1=C(Cl)C=C2NC(CSCC3=CC=CC=C3)=NS(=O)(=O)C2=C1

Độ tan chảy

210-211

Độ hòa tan

8.91 mg/L

logP

1.73

logS

-4.5

pKa (strongest acidic)

8.77

pKa (Strongest Basic)

1.25

PSA

118.69 Å²

Refractivity

104.14 m³·mol^-1

Polarizability

41.5 Å³

Rotatable Bond Count

H Bond Acceptor Count

H Bond Donor Count

Physiological Charge

Number of Rings

Bioavailability

Rule of Five

true

Ghose Filter

true

pKa

Dược Lực Học : Benzthiazide is used to treat hypertension and edema. Like other thiazides, benzthiazide promotes water loss from the body (diuretics). They inhibit Na⁺/Cl^- reabsorption from the distal convoluted tubules in the kidneys. Thiazides also cause loss of potassium and an increase in serum uric acid. Thiazides are often used to treat hypertension, but their hypotensive effects are not necessarily due to their diuretic activity. Thiazides have been shown to prevent hypertension-related morbidity and mortality although the mechanism is not fully understood. Thiazides cause vasodilation by activating calcium-activated potassium channels (large conductance) in vascular smooth muscles and inhibiting various carbonic anhydrases in vascular tissue.

Cơ Chế Tác Dụng : Benzthiazide is used to treat hypertension and edema. Like other thiazides, benzthiazide promotes water loss from the body (diuretics). They inhibit Na+/Cl- reabsorption from the distal convoluted tubules in the kidneys. Thiazides also cause loss of potassium and an increase in serum uric acid. Thiazides are often used to treat hypertension, but their hypotensive effects are not necessarily due to their diuretic activity. Thiazides have been shown to prevent hypertension-related morbidity and mortality although the mechanism is not fully understood. Thiazides cause vasodilation by activating calcium-activated potassium channels (large conductance) in vascular smooth muscles and inhibiting various carbonic anhydrases in vascular tissue. As a diuretic, benzthiazide inhibits active chloride reabsorption at the early distal tubule via the Na-Cl cotransporter, resulting in an increase in the excretion of sodium, chloride, and water. Thiazides like benzthiazide also inhibit sodium ion transport across the renal tubular epithelium through binding to the thiazide sensitive sodium-chloride transporter. This results in an increase in potassium excretion via the sodium-potassium exchange mechanism. The antihypertensive mechanism of benzthiazide is less well understood although it may be mediated through its action on carbonic anhydrases in the smooth muscle or through its action on the large-conductance calcium-activated potassium (KCa) channel, also found in the smooth muscle.

Dược Động Học :

▧ Absorption :
Absorbed in the digestive tract.
▧ Protein binding :
30%

Độc Tính : Symptoms of overdose include nausea, vomiting, fatigue, urinary problems and drowsiness.

Chỉ Định : For the treatment of high blood pressure and management of edema.

Tương Tác Thuốc :

Digoxin Possible electrolyte variations and arrhythmias
Lithium The thiazide diuretic, benzthiazide, may increase serum levels of lithium.

Dữ Kiện Thương Mại

Nhà Sản Xuất

Công ty :

Sản phẩm biệt dược : Aquatag
Công ty :

Sản phẩm biệt dược : Dihydrex
Công ty :

Sản phẩm biệt dược : Diucen
Công ty :

Sản phẩm biệt dược : Edemax
Công ty :

Sản phẩm biệt dược : Exna
Công ty :

Sản phẩm biệt dược : Foven

Tài Liệu Tham Khảo Thêm

drugbank

http://www.drugbank.ca/drugs/DB00562

PubChem Compound

http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2343

PubChem Substance

http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506752

KEGG Compound

http://www.genome.jp/dbget-bin/www_bget?cpd:C07759

KEGG Drug

http://www.genome.jp/dbget-bin/www_bget?drug:D00651

ChemSpider

http://www.chemspider.com/Chemical-Structure.2253.html

PharmGKB

http://www.pharmgkb.org/drug/PA164776841

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