Tìm theo
Fenoldopam
Các tên gọi khác (4 ) :
  • Fenoldopam
  • Fénoldopam
  • Fenoldopam
  • Fenoldopamum
antihypertensive agents, vasodilator agents, dopamine agonists
Thuốc Gốc
Small Molecule
CAS: 67227-57-0
ATC: C01CA19
ĐG : Baxter International Inc. , http://www.baxter.com
CTHH: C16H16ClNO3
PTK: 305.756
A dopamine D1 receptor agonist that is used as an antihypertensive agent. It lowers blood pressure through arteriolar vasodilation. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C16H16ClNO3
Phân tử khối
305.756
Monoisotopic mass
305.08187109
InChI
InChI=1S/C16H16ClNO3/c17-15-11-5-6-18-8-13(9-1-3-10(19)4-2-9)12(11)7-14(20)16(15)21/h1-4,7,13,18-21H,5-6,8H2
InChI Key
InChIKey=TVURRHSHRRELCG-UHFFFAOYSA-N
IUPAC Name
6-chloro-1-(4-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol
Traditional IUPAC Name
fenoldopam
SMILES
OC1=CC=C(C=C1)C1CNCCC2=C(Cl)C(O)=C(O)C=C12
Độ hòa tan
4000 mg/L
logP
2
logS
-3
pKa (strongest acidic)
8.12
pKa (Strongest Basic)
10.4
PSA
72.72 Å2
Refractivity
82.68 m3·mol-1
Polarizability
30.71 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
4
H Bond Donor Count
4
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Fenoldopam is an agonist at D1-like dopamine receptors, binds to α2-adrenoceptors, increasing renal blood flow.
Cơ Chế Tác Dụng : A dopamine D1 receptor agonist that is used as an antihypertensive agent. It lowers blood pressure through arteriolar vasodilation. [PubChem] Fenoldopam is a rapid-acting vasodilator. It is an agonist for D1-like dopamine receptors and binds with moderate affinity to α2-adrenoceptors. It has no significant affinity for D2-like receptors, α1 and β-adrenoceptors, 5HT1 and 5HT2 receptors, or muscarinic receptors. Fenoldopam is a racemic mixture with the R-isomer responsible for the biological activity. The R-isomer has approximately 250-fold higher affinity for D1-like receptors than does the S-isomer. In non-clinical studies, fenoldopam had no agonist effect on presynaptic D2-like dopamine receptors, or α or β -adrenoceptors, nor did it affect angiotensin-converting enzyme activity. Fenoldopam may increase norepinephrine plasma concentration.
Dược Động Học :

▧ Metabolism :
Elimination is largely by conjugation, without participation of cytochrome P-450 enzymes. Methylation, glucuronidation, and sulfation are the main routes of conjugation.
▧ Route of Elimination :
Radiolabeled studies show that about 90% of infused fenoldopam is eliminated in urine, 10% in feces. Elimination is largely by conjugation, without participation of cytochrome P-450 enzymes. Only 4% of the administered dose is excreted unchanged.
▧ Half Life :
The elimination half-life is about 5 minutes in mild to moderate hypertensives, with little difference between the R (active) and S isomers.
Độc Tính : The most likely reaction of overdose would be excessive hypotension which should be treated with drug discontinuation and appropriate supportive measures.
Chỉ Định : For the in-hospital, short-term (up to 48 hours) management of severe hypertension when rapid, but quickly reversible, emergency reduction of blood pressure is clinically indicated, including malignant hypertension with deteriorating end-organ function.
Liều Lượng & Cách Dùng : Injection, solution - Intravenous drip
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Hospira
    Sản phẩm biệt dược : Corlopam
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00800
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3341
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504963
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00613
ChemSpider
http://www.chemspider.com/Chemical-Structure.3224.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/55390-071-01
PharmGKB
http://www.pharmgkb.org/drug/PA164784034
Wikipedia
http://en.wikipedia.org/wiki/Fenoldopam
RxList
http://www.rxlist.com/cgi/generic3/fenoldopam.htm
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