Tìm theo
Temocapril
Các tên gọi khác (1) :
  • Temocaprilum
angiotensin converting enzyme inhibitors, antihypertensive agents
Thuốc Gốc
Small Molecule
CAS: 111902-57-9
ATC: C09AA14
CTHH: C23H29ClN2O5S2
PTK: 513.07
Temocapril is a prodrug-type angiotensin-I converting enzyme (ACE) inhibitor not approved for use in the United States, but is approved in Japan and South Korea. Temocapril can also be used in hemodialysis patients without risk of serious accumulation.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C23H29ClN2O5S2
Phân tử khối
513.07
Monoisotopic mass
512.120641135
InChI
InChI=1/C23H28N2O5S2.ClH/c1-2-30-23(29)17(11-10-16-7-4-3-5-8-16)24-18-15-32-20(19-9-6-12-31-19)13-25(22(18)28)14-21(26)27;/h3-9,12,17-18,20,24H,2,10-11,13-15H2,1H3,(H,26,27);1H/t17-,18-,20-;/s2
InChI Key
InChIKey=XDDQNOKKZKHBIX-ZXTPIAIONA-N
IUPAC Name
2-[(2S,6R)-6-{[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino}-5-oxo-2-(thiophen-2-yl)-1,4-thiazepan-4-yl]acetic acid hydrochloride
Traditional IUPAC Name
[(2S,6R)-6-{[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino}-5-oxo-2-(thiophen-2-yl)-1,4-thiazepan-4-yl]acetic acid hydrochloride
SMILES
Cl.CCOC(=O)[C@H](CCC1=CC=CC=C1)N[C@H]1CS[C@@H](CN(CC(O)=O)C1=O)C1=CC=CS1
Độ tan chảy
decomposes at 187
Độ hòa tan
<1 mg/mL
logP
2.04
logS
-5.1
pKa (strongest acidic)
3.88
pKa (Strongest Basic)
5.14
PSA
95.94 Å2
Refractivity
124.1 m3·mol-1
Polarizability
49.28 Å3
Rotatable Bond Count
11
H Bond Acceptor Count
5
H Bond Donor Count
2
Physiological Charge
-1
Number of Rings
3
Bioavailability
0
MDDR-Like Rule
true
Dược Lực Học : Temocapril is a prodrug of its active metabolite (and diacid form) temocaprilat which contains a thiazepine ring. Temocaprilat has slightly higher potency than enalaprilat in ACE inhibition isolated from rabbit lung. ACE inhibitors exert their hemodynamic effect mainly by inhibiting the renin-angiotensin system. They also modulate sympathetic nervous system activity and increase prostaglandin synthesis. They cause mainly vasodilation and mild natriuresis without affecting heart rate and contractility.). When compared with other Angiotensin-converting Enzyme Inhibitors, temocapril's advantages include a rapid onset of action and what research suggests is tighter vascular ACE binding than enalaprilat.
Dược Động Học :
▧ Absorption :
Temocapril is rapidly absorbed in the gastrointestinal tract and converted into the diacid (active) metabolite, which inhibits ACE in plasma.
▧ Protein binding :
99.5%, including those with renal impairment.
▧ Route of Elimination :
Temocapril is eliminated primarily through the liver and kidneys.
▧ Half Life :
13.1 hours in patients with normal liver function.
▧ Clearance :
19.4% urinary recovery.
Độc Tính : In rats, whether or male or female, the LD50 values of temocapril were higher than 5000 mg/kg.
Chỉ Định : Temocapril is an ACE inhibitor primarily indicated in the treatment of hypertension and congestive heart failure, diabetic nephropathy, and improvement of prognosis for coronary artery diseases (including acute myocardial infarction).
Liều Lượng & Cách Dùng : Tablet - Oral - 1 mg
Tablet - Oral - 2 mg
Tablet - Oral - 4 mg
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Sankyo
    Sản phẩm biệt dược : Acecol
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB08836
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D08566
Wikipedia
http://en.wikipedia.org/wiki/Temocapril
Drugs.com
http://www.drugs.com/international/temocapril.html
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