Details
Stereochemistry | ACHIRAL |
Molecular Formula | C11H14N4O4 |
Molecular Weight | 266.2533 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1C2=C(N(CC3OCCO3)C=N2)C(=O)N(C)C1=O
InChI
InChIKey=HWXIGFIVGWUZAO-UHFFFAOYSA-N
InChI=1S/C11H14N4O4/c1-13-9-8(10(16)14(2)11(13)17)15(6-12-9)5-7-18-3-4-19-7/h6-7H,3-5H2,1-2H3
Molecular Formula | C11H14N4O4 |
Molecular Weight | 266.2533 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/?term=11268710Curator's Comment: description was created based on several sources, including
http://cathaydrug.ph/product/dilatair/
https://www.ncbi.nlm.nih.gov/pubmed/18376093
Sources: https://www.ncbi.nlm.nih.gov/pubmed/?term=11268710
Curator's Comment: description was created based on several sources, including
http://cathaydrug.ph/product/dilatair/
https://www.ncbi.nlm.nih.gov/pubmed/18376093
Doxofylline (7-(1, 3-dioxalan-2-ylmethyl) theophylline) is a novel xanthine bronchodilator which differs from theophylline in that it contains a dioxalane group in position 7. Doxofylline is indicated for the treatment of bronchial asthma, pulmonary disease with spastic bronchial component and Chronic Obstructive Pulmonary Disease (COPD). Doxofylline does not directly inhibit any of the known HDAC enzymes, and did not inhibit any phosphodiesterase (PDE) enzyme sub types or act as an antagonist at any of the known adenosine receptors, except for PDE2A(1), and adenosine A(2A) and only at the highest tested concentration (10(-4) M). Doxofylline has greatly decreased affinity towards adenosine A1 and A2 receptors, which explain its better safety profile. Moreover, it does not interfere with calcium influx into the cells nor antagonize calcium channel blockers. Doxofylline has been shown to be a more potent bronchodilator with fewer side effects than theophylline. This drug should not be administered together with other xanthine derivatives, including beverages and foods containing caffeine.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL2652 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22138191 |
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Target ID: CHEMBL251 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22138191 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Palliative | Dilatair Approved UseUnknown |
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Palliative | Ddilatair Approved UseUnknown |
PubMed
Title | Date | PubMed |
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Doxofylline and respiratory mechanics. Short-term effects in mechanically ventilated patients with airflow obstruction and respiratory failure. | 1989 Oct |
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Doxofylline: a new generation xanthine bronchodilator devoid of major cardiovascular adverse effects. | 2001 |
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Conclusion without support - remarks on 'Efficacy and safely of doxyphyllin compared to Theophylline in chronic reversible asthma- a double-blind randomized placebo-controlled multicentre trial' by Goldstein MF, Chervinsky P (published in MedSciMonit, 2002; 8(4):CR297-304. | 2002 Aug |
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[Clinical study on doxofylline injection in treatment of children with acute asthma attacks]. | 2004 Feb |
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Doxofylline: The next generation methylxanthine. | 2008 Mar |
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[Effects of tetramethylpyrazine on fractalkine and tumor necrosis factor-alpha expression in patients with chronic pulmonary heart disease]. | 2010 Apr |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: http://cathaydrug.ph/product/dilatair/
Elderly Patients: 200 mg tablet two or three times daily.
Adults: 400 mg tablet two or three times daily.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/2776832
Curator's Comment: Doxofylline inhibited PAF-induced bronchoconstriction in vitro, and the concomitant generation of TXA2-like activity in perfused guinea-pig lungs.
Unknown
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 18:54:49 UTC 2023
by
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on
Fri Dec 15 18:54:49 UTC 2023
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Record UNII |
MPM23GMO7Z
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Record Status |
Validated (UNII)
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WHO-VATC |
QR03DA11
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FDA ORPHAN DRUG |
399413
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NCI_THESAURUS |
C744
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WHO-ATC |
R03DA11
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m4756
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DOXOFYLLINE
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C76317
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CHEMBL1527608
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274-239-6
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SUB06390MIG
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