Details
Stereochemistry | ACHIRAL |
Molecular Formula | 8C9H10N4O4.7C4H10N2 |
Molecular Weight | 2508.55 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
C1CNCCN1.C2CNCCN2.C3CNCCN3.C4CNCCN4.C5CNCCN5.C6CNCCN6.C7CNCCN7.CN8C9=C(N(CC(O)=O)C=N9)C(=O)N(C)C8=O.CN%10C%11=C(N(CC(O)=O)C=N%11)C(=O)N(C)C%10=O.CN%12C%13=C(N(CC(O)=O)C=N%13)C(=O)N(C)C%12=O.CN%14C%15=C(N(CC(O)=O)C=N%15)C(=O)N(C)C%14=O.CN%16C%17=C(N(CC(O)=O)C=N%17)C(=O)N(C)C%16=O.CN%18C%19=C(N(CC(O)=O)C=N%19)C(=O)N(C)C%18=O.CN%20C%21=C(N(CC(O)=O)C=N%21)C(=O)N(C)C%20=O.CN%22C%23=C(N(CC(O)=O)C=N%23)C(=O)N(C)C%22=O
InChI
InChIKey=IUKJNIOSXCPLLP-UHFFFAOYSA-N
InChI=1S/8C9H10N4O4.7C4H10N2/c8*1-11-7-6(8(16)12(2)9(11)17)13(4-10-7)3-5(14)15;7*1-2-6-4-3-5-1/h8*4H,3H2,1-2H3,(H,14,15);7*5-6H,1-4H2
Acefylline is a stimulant drug of the xanthine chemical class. It acts as an adenosine receptor antagonist. Acephylline piperazine is a theophylline derivative with a direct bronchodilator action. It has the advantages over theophylline in being far less toxic and producing minimal gastric irritation. It is indicated for the treatment of asthma, emphysema, acute and chronic bronchitis associated with bronchospasm.Acefylline relaxes smooth muscles, relieves bronchospasm & has a stimulant effect on respiration. It stimulates the myocardium & central nervous system, decreases peripheral resistance & venous pressure & causes diuresis. The mechanism of action is still not clear, inhibition of phosphodiesterase with a resulting increase in intracellular cyclic AMP does occur, but not apparently at concentrations normally used for clinical effect. Other proposed mechanisms of action include adenosine receptor antagonism, prostaglandin antagonism & effects on intracellular calcium. Sodium phenobarbital is a non-selective central nervous system depressant that is primarily used as sedative-hypnotic.
CNS Activity
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL255 |
27.6 µM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | Etaphylline Approved UseEtaphylline is primarily indicated in conditions like Bronchitis, Bronchospasm, Emphysema, and can also be given in adjunctive therapy as an alternative drug of choice in Asthma, Biliary colic, Cardiac insufficiency. |
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Primary | Etaphylline Approved UseEtaphylline is primarily indicated in conditions like Bronchitis, Bronchospasm, Emphysema, and can also be given in adjunctive therapy as an alternative drug of choice in Asthma, Biliary colic, Cardiac insufficiency. |
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Primary | Etaphylline Approved UseEtaphylline is primarily indicated in conditions like Bronchitis, Bronchospasm, Emphysema, and can also be given in adjunctive therapy as an alternative drug of choice in Asthma, Biliary colic, Cardiac insufficiency. |
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Primary | Etaphylline Approved UseEtaphylline is primarily indicated in conditions like Bronchitis, Bronchospasm, Emphysema, and can also be given in adjunctive therapy as an alternative drug of choice in Asthma, Biliary colic, Cardiac insufficiency. |
PubMed
Title | Date | PubMed |
---|---|---|
Development and validation of chemometrics-assisted spectrophotometric and liquid chromatographic methods for the simultaneous determination of two multicomponent mixtures containing bronchodilator drugs. | 2007 Feb 19 |
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Solid-state chemistry of ambroxol theophylline-7-acetate. | 2007 May |
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Molecularly imprinted polymers for ochratoxin a extraction and analysis. | 2010 Jun |
Patents
Sample Use Guides
In Vivo Use Guide
Curator's Comment: Can be used orally: Dosage:
2 to 6 tablets daily, in several doses at regular intervals during the day.
Composition:
Each coated tablet contains: - Acefylline piperazine 0.250 g http://www.unipharma-sy.com/en/MedicineView/48/142/ETAPHYLLINE_.aspx
Dosage & route of administration & duration:
The optimum therapeutic serum concentration is considered to range from 10 to 20 mcg/ml
To avoid adverse effects the rate of infusion administration should not exceed 20 mg / min
For I.M & slow I.V injection of 200 mg over at least 15 min.
For IV infusion a loading dose of 4 mg/kg may be given over 20 to 30 min followed by a suggested maintenance dose of 0.5 mg /kg / hour reduced after 12 hours to 0.4 mg/kg/hour.
Suggested Doses for children:
4mg/Kg by slow IV injection over at least 15 min or by infusion with a loading dose of 4 mg/kg followed by maintenance doses of:
Children from 6 months to 6 years...................0.8 to 1 mg/kg/hour, reduced after the first 12 hours to 0.6 mg/kg/hour.
Children over 6 years.....................................0.75 mg/kg/hour, reduced after the first 12 hours to 0.5 mg/kg/hour.
Route of Administration:
Parenteral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26616205
After topical application of a gel formulation containing 3% acefylline at the surface of reconstructed human epidermis, immunoblotting analysis showed an increase in the total amount of deiminated proteins, and confocal microscopy showed an enhanced deimination in the stratum corneum. This demonstrated the activation of PADs in living cells.
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NCI_THESAURUS |
C319
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QR03DA09
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WHO-ATC |
R03DA09
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18833-13-1
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SUB12706MIG
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ACTIVE MOIETY
PARENT (SALT/SOLVATE)
SUBSTANCE RECORD