Tìm theo
Debrisoquin
Các tên gọi khác (6 ) :
  • Debrisochinum
  • Debrisoquin
  • Debrisoquina
  • Debrisoquine
  • Debrisoquinum
  • Isocaramidine
antihypertensive agents, adrenergic agents, sympatholytics
Thuốc Gốc
Small Molecule
CAS: 1131-64-2
ATC: C02CC04
CTHH: C10H13N3
PTK: 175.2303
An adrenergic neuron-blocking drug similar in effects to guanethidine. It is also noteworthy in being a substrate for a polymorphic cytochrome P-450 enzyme. Persons with certain isoforms of this enzyme are unable to properly metabolize this and many other clinically important drugs. They are commonly referred to as having a debrisoquin 4-hydroxylase polymorphism. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C10H13N3
Phân tử khối
175.2303
Monoisotopic mass
175.110947431
InChI
InChI=1S/C10H13N3/c11-10(12)13-6-5-8-3-1-2-4-9(8)7-13/h1-4H,5-7H2,(H3,11,12)
InChI Key
InChIKey=JWPGJSVJDAJRLW-UHFFFAOYSA-N
IUPAC Name
1,2,3,4-tetrahydroisoquinoline-2-carboximidamide
Traditional IUPAC Name
debrisoquin
SMILES
NC(=N)N1CCC2=CC=CC=C2C1
Độ tan chảy
278-280 °C
Độ hòa tan
8.42e-01 g/l
logP
0.75
logS
-2.3
pKa (Strongest Basic)
12.47
PSA
53.11 Å2
Refractivity
63.85 m3·mol-1
Polarizability
19.48 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
3
H Bond Donor Count
2
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Debrisoquin is an adrenergic neuron-blocking drug similar in effects to guanethidine. It is a substrate for a polymorphic cytochrome P-450 enzyme. Persons with certain isoforms of this enzyme are unable to properly metabolize this and many other clinically important drugs. They are commonly referred to as having a debrisoquin 4-hydroxylase polymorphism.
Cơ Chế Tác Dụng : An adrenergic neuron-blocking drug similar in effects to guanethidine. It is also noteworthy in being a substrate for a polymorphic cytochrome P-450 enzyme. Persons with certain isoforms of this enzyme are unable to properly metabolize this and many other clinically important drugs. They are commonly referred to as having a debrisoquin 4-hydroxylase polymorphism. [PubChem] Debrisoquin acts at the sympathetic neuroeffector junction by inhibiting or interfering with the release and/or distribution of norepinephrine, rather than acting at the effector cell by inhibiting the association of norepinephrine with its receptors. It is taken up by norepinephrine transporters. It becomes concentrated in NE transmitter vesicles, replacing NE in these vesicles. This leads to a gradual depletion of NE stores in the nerve endings. Once inside the terminal it blocks the release of noradrenaline in response to arrival of an action potential. In contrast to ganglionic blocking agents, debrisoquin suppresses equally the responses mediated by alpha-and beta-adrenergic receptors but does not produce parasympathetic blockade. Since sympathetic blockade results in modest decreases in peripheral resistance and cardiac output, debrisoquin lowers blood pressure in the supine position. It further reduces blood pressure by decreasing the degree of vasoconstriction that normally results from reflex sympathetic nervous activity upon assumption of the upright posture, thus reducing venous return and cardiac output more.
Dược Động Học :

▧ Metabolism :
Hepatic.
Chỉ Định : For the treatment of moderate and severe hypertension, either alone or as an adjunct, and for the treatment of renal hypertension.
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : lkapharm
    Sản phẩm biệt dược : Bonipress
  • Công ty : Roche
    Sản phẩm biệt dược : Declinax
  • Công ty : Chinoin
    Sản phẩm biệt dược : Tendor
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB04840
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2966
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507664
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C13650
ChemSpider
http://www.chemspider.com/Chemical-Structure.2860.html
PharmGKB
http://www.pharmgkb.org/drug/PA452616
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