Tìm theo
Guanabenz
Các tên gọi khác (7 ) :
  • Guanabenz
  • Guanabenzo
  • Guanabenzum
  • SID26665151
  • SID26751943
  • WY-8678
  • Wytensin
antihypertensive agents, adrenergic alpha 2 receptor agonists
Thuốc Gốc
Small Molecule
CAS: 5051-62-7
ĐG : Ivax Pharmaceuticals
CTHH: C8H8Cl2N4
PTK: 231.082
An alpha-2 selective adrenergic agonist used as an antihypertensive agent. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Phân tử khối
231.082
Monoisotopic mass
230.01260169
InChI
InChI=1S/C8H8Cl2N4/c9-6-2-1-3-7(10)5(6)4-13-14-8(11)12/h1-4H,(H4,11,12,14)/b13-4+
InChI Key
InChIKey=WDZVGELJXXEGPV-YIXHJXPBSA-N
IUPAC Name
2-{[(2,6-dichlorophenyl)methylidene]amino}guanidine
Traditional IUPAC Name
2-{[(2,6-dichlorophenyl)methylidene]amino}guanidine
SMILES
NC(N)=NN=CC1=C(Cl)C=CC=C1Cl
Độ tan chảy
225-227
Độ hòa tan
8.89e-02 g/l
logP
3.2
logS
-3.4
pKa (Strongest Basic)
6.82
PSA
76.76 Å2
Refractivity
58.15 m3·mol-1
Polarizability
21.58 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
4
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
caco2 Permeability
-4.5
Dược Lực Học : Guanabenz, a centrally acting α-2 adrenergic agonist, is indicated for treatment of hypertension.
Cơ Chế Tác Dụng : An alpha-2 selective adrenergic agonist used as an antihypertensive agent. [PubChem] Guanabenz's antihypertensive effect is thought to be due to central alpha-adrenergic stimulation, which results in a decreased sympathetic outflow to the heart, kidneys, and peripheral vasculature in addition to a decreased systolic and diastolic blood pressure and a slight slowing of pulse rate. Chronic administration of guanabenz also causes a decrease in peripheral vascular resistance.
Dược Động Học :
▧ Absorption :
Approximately 75% absorbed from gastrointestinal tract
▧ Protein binding :
90%
▧ Metabolism :
Hepatic
▧ Half Life :
6 hours.
Độc Tính : Excessive contraction of the pupils, irritability, low blood pressure, sleepiness, slow heartbeat, sluggishness
Chỉ Định : For management of High blood pressure
Tương Tác Thuốc :
  • Thiabendazole The strong CYP1A2 inhibitor, Thiabendazole, may increase the effects and toxicity of Guanabenz by decreasing Guanabenz metabolism and clearance. Monitor for changes in the therapeutic and adverse effects of Guanabenz if Thiabendazole is initiated, discontinued or dose changed.
  • Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
  • Trimipramine Trimipramine may reduce the antihypertensive effect of the alpha2-agonist, Guanabenz. Trimipramine may also increase the rebound hypertensive effect of Clonidine. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Clonidine if Trimipramine is initiated, discontinued or dose changed. Guanabenz should be withdrawn very gradually to reduce the risk of hypertensive crisis.
Dữ Kiện Thương Mại
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