Tìm theo
Nedocromil
Các tên gọi khác (5 ) :
  • 9-Ethyl-6,9-dihydro-4,6-dioxo-10-propyl-4H-pyrano(3,2-g)chinolin-2,8-dicarbonsaeure
  • 9-Ethyl-6,9-dihydro-4,6-dioxo-10-propyl-4H-pyrano(3,2-g)quinoline-2,8-dicarboxylic acid
  • Nedocromil
  • Nedocromilo
  • Nedocromilum
Thuốc chống dị ứng
Thuốc Gốc
Small Molecule
CAS: 69049-73-6
ATC: R01AC07, R03BC03, S01GX04
ĐG : Allergan Inc. , http://www.allergan.com
CTHH: C19H17NO7
PTK: 371.3408
A pyranoquinolone derivative that inhibits activation of inflammatory cells which are associated with asthma, including eosinophils, neutrophils, macrophages, mast cells, monocytes, and platelets. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C19H17NO7
Phân tử khối
371.3408
Monoisotopic mass
371.100501903
InChI
InChI=1S/C19H17NO7/c1-3-5-9-16-10(13(21)7-12(18(23)24)20(16)4-2)6-11-14(22)8-15(19(25)26)27-17(9)11/h6-8H,3-5H2,1-2H3,(H,23,24)(H,25,26)
InChI Key
InChIKey=RQTOOFIXOKYGAN-UHFFFAOYSA-N
IUPAC Name
9-ethyl-4,6-dioxo-10-propyl-4H,6H,9H-chromeno[7,6-b]pyridine-2,8-dicarboxylic acid
Traditional IUPAC Name
nedocromil
SMILES
CCCC1=C2N(CC)C(=CC(=O)C2=CC2=C1OC(=CC2=O)C(O)=O)C(O)=O
Độ tan chảy
299 dec °C
Độ hòa tan
145 mg/L
logP
2.22
logS
-3.9
pKa (strongest acidic)
2.28
pKa (Strongest Basic)
-4.2
PSA
121.21 Å2
Refractivity
98.09 m3·mol-1
Polarizability
36.95 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
8
H Bond Donor Count
2
Physiological Charge
-2
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Nedocromil is a anti-inflammatory agent and can be administered directly to the bronchial mucosa. It has significant inhibitory effect on allergen-induced early and late asthmatic reactions and on bronchial hyperresponsiveness.
Cơ Chế Tác Dụng : A pyranoquinolone derivative that inhibits activation of inflammatory cells which are associated with asthma, including eosinophils, neutrophils, macrophages, mast cells, monocytes, and platelets. [PubChem] Nedocromil has been shown to inhibit the in vitro activation of, and mediator release from, a variety of inflammatory cell types associated with asthma, including eosinophils, neutrophils, macrophages, mast cells, monocytes, and platelets. Nedocromil inhibits activation and release of inflammatory mediators such as histamine, prostaglandin D2 and leukotrienes c4 from different types of cells in the lumen and mucosa of the bronchial tree. These mediators are derived from arachidonic acid metabolism through the lipoxygenase and cyclo-oxygenase pathways. The mechanism of action of nedocromil may be due partly to inhibition of axon reflexes and release of sensory neuropeptides, such as substance P, neurokinin A, and calcitonin-geneñrelated peptides. The result is inhibition of bradykinin-induced bronchoconstriction. Nedocromil does not posess any bronchodilator, antihistamine, or corticosteroid activity.
Dược Động Học :
▧ Absorption :
Low
▧ Protein binding :
approximately 89% protein bound in human plasma over a concentration range of 0.5 to 50 µg/mL
▧ Metabolism :
Nedocromil is not metabolized after IV administration and is excreted unchanged.
▧ Route of Elimination :
It is not metabolized and is eliminated primarily unchanged in urine (70%) and feces (30%).
▧ Half Life :
~3.3 hours
Độc Tính : Side effects include headache, nasal congestion, ocular burning, irritation and stinging, unpleasant taste, cough, difficulty breathing, noisy breathing, shortness of breath, tightness in chest, wheezing, conjunctivitis, blurred vision, change in color vision, difficulty seeing at night, increased sensitivity of eyes to sunlight.
Chỉ Định : For the treatment of mild to moderate asthma
Liều Lượng & Cách Dùng : Liquid - Ophthalmic
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Alocril
  • Công ty :
    Sản phẩm biệt dược : Tilade
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00716
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=50294
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507587
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07255
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D05129
ChemSpider
http://www.chemspider.com/Chemical-Structure.45608.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0023-8842-05
PharmGKB
http://www.pharmgkb.org/drug/PA450601
Wikipedia
http://en.wikipedia.org/wiki/Nedocromil
RxList
http://www.rxlist.com/cgi/generic3/nedocr.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/til1444.shtml
Drugs.com
http://www.drugs.com/cdi/nedocromil-drops.html
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