Tìm theo
Amlexanox
Các tên gọi khác (5 ) :
  • 2-Amino-7-isopropyl-5-oxo-5H-(1)benzopyrano(2,3-b)pyridine-3-carboxylic acid
  • Amlexanox
  • Amlexanoxo
  • Amlexanoxum
  • Amoxanox
Thuốc chống dị ứng
Thuốc Gốc
Small Molecule
CAS: 68302-57-8
ATC: A01AD07, R03DX01
ĐG : Block Drug Corp.
CTHH: C16H14N2O4
PTK: 298.2934
Amlexanox is an antiallergic drug, clinically effective for atopic diseases, especially allergic asthma and rhinitis. Amlexanox as a topical paste is a well tolerated treatment of recurrent aphthous ulcers. Recurrent aphthous ulcer (RAU) is the most prevalent oral mucosal disease in humans, estimated to affect between 5% and 50% of the general population.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C16H14N2O4
Phân tử khối
298.2934
Monoisotopic mass
298.095356946
InChI
InChI=1S/C16H14N2O4/c1-7(2)8-3-4-12-9(5-8)13(19)10-6-11(16(20)21)14(17)18-15(10)22-12/h3-7H,1-2H3,(H2,17,18)(H,20,21)
InChI Key
InChIKey=SGRYPYWGNKJSDL-UHFFFAOYSA-N
IUPAC Name
2-amino-5-oxo-7-(propan-2-yl)-5H-chromeno[2,3-b]pyridine-3-carboxylic acid
Traditional IUPAC Name
amlexanox
SMILES
CC(C)C1=CC2=C(OC3=NC(N)=C(C=C3C2=O)C(O)=O)C=C1
Độ hòa tan
1.46e-01 g/l
logP
4.1
logS
-3.3
pKa (strongest acidic)
4.3
pKa (Strongest Basic)
0.87
PSA
102.51 Å2
Refractivity
81.43 m3·mol-1
Polarizability
30.82 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
5
H Bond Donor Count
2
Physiological Charge
-1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Amlexanox is a mucoadhesive oral paste which has been clinically proven to abort the onset, accelerate healing and resolve the pain of aphthous ulcers (canker sores). It decreases the time ulcers take to heal. Because amlexanox decreases the healing time, it also decreases the pain you feel. Recent studies have also shown that the majority of ulcers can be prevented by application of the paste during the prodromal (pre-ulcerative) phase of the disease. Recurrent Aphthous Ulcers (RAU) also known as Recurrent Aphthous Stomatitis (RAS) is recognized as the most common oral mucosal disease known to man. Estimates suggest that 20% - 25% of the general population suffer at least one incidence of aphthous ulcers each year. Amlexanox is also being investigated for its anti-allergenic and anti-inflammatory properties.
Cơ Chế Tác Dụng : Amlexanox is an antiallergic drug, clinically effective for atopic diseases, especially allergic asthma and rhinitis. Amlexanox as a topical paste is a well tolerated treatment of recurrent aphthous ulcers. Recurrent aphthous ulcer (RAU) is the most prevalent oral mucosal disease in humans, estimated to affect between 5% and 50% of the general population. As a benzopyrano-bipyridine carboxylic acid derivative, amlexanox has anti-inflammatory and antiallergic properties. It inhibits chemical mediatory release of the slow-reacting substance of anaphylaxis (SRS-A) and may have antagonistic effects on interleukin-3. When cells are under stress, they release an inactive form of human fibroblast growth factor 1 (FGF-1), a potent mitogen (entity that causes mitosis). Amlexanox binds to FGF1, increasing its conformational stability, sterically blocking Cu(2+) induced oxidation which normally leads to activation of FGF-1.
Dược Động Học :
▧ Absorption :
No significant absorption directly through the active ulcer. Most of the systemic absorption is via the gastrointestinal tract.
▧ Metabolism :
Metabolized to hydroxylated and conjugated metabolites.
▧ Half Life :
Elimination half-life is 3.5 ± 1.1 hours.
Chỉ Định : Used as a paste in the mouth to treat aphthous ulcers (canker sores).
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Aphthasol
  • Công ty :
    Sản phẩm biệt dược : Elics
  • Công ty :
    Sản phẩm biệt dược : OraDisc A
  • Công ty :
    Sản phẩm biệt dược : Solfa
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01025
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2161
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504508
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01828
ChemSpider
http://www.chemspider.com/Chemical-Structure.2076.html
PharmGKB
http://www.pharmgkb.org/drug/PA164745310
Drugs.com
http://www.drugs.com/cdi/amlexanox.html
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