Theophylline

Not A/B H target. Theophylline is a natural alkaloid dimethylxanthine derivative of xanthine isolated from the plants Camellia sinensis and Coffea arabica, green and black tea. Theophylline appears to inhibit phosphodiesterase and prostaglandin production, regulate calcium flux and intracellular calcium distribution, and antagonize adenosine. Physiologically, this agent relaxes bronchial smooth muscle, produces vasodilation (except in cerebral vessels), stimulates the CNS, stimulates cardiac muscle, induces diuresis, and increases gastric acid secretion; it may also suppress inflammation and improve contractility of the diaphragm. Theophylline played an important role in the management of both acute and chronic reversible airway obstruction, in particular asthma and chronic bronchitis. However, it has a narrow safety window, which, along with its variability in disposition, makes dosing difficult to predict and toxicity difficult to prevent. Symptoms of toxicity include tachycardia, severe restlessness, agitation, nausea and vomiting, particularly at high blood concentrations

General

Type : Alkaloid,Natural,Purine,Not A\/B H target

Chemical_Nomenclature : 1,3-dimethyl-7H-purine-2,6-dione

Canonical SMILES : CN1C2=C(C(=O)N(C1=O)C)NC=N2

InChI : InChI=1S\/C7H8N4O2\/c1-10-5-4(8-3-9-5)6(12)11(2)7(10)13\/h3H,1-2H3,(H,8,9)

InChIKey : ZFXYFBGIUFBOJW-UHFFFAOYSA-N

Other name(s) : 1,3-Dimethylxanthine,Theophyllin,Elixophyllin,CHEMBL190,CHEBI:28177,ZINC18043251,DB-053224


MW : 180.16

Formula : C7H8N4O2

CAS_number : 58-55-9

PubChem : 2153

UniChem : ZFXYFBGIUFBOJW-UHFFFAOYSA-N

IUPHAR :

Wikipedia :

Target

Families : Theophylline ligand of proteins in family: Pectinacetylesterase-Notum

Stucture : 6TUZ Theophylline- human Notum complex

Protein : human-NOTUM

References (11)

Title : Low-dose theophylline does not exert its anti-inflammatory effects in mild asthma through upregulation of interleukin-10 in alveolar macrophages - Oliver_2001_Allergy_56_1087
Author(s) : Oliver B , Tomita K , Keller A , Caramori G , Adcock I , Chung KF , Barnes PJ , Lim S
Ref : Allergy , 56 :1087 , 2001
Abstract : Oliver_2001_Allergy_56_1087
ESTHER : Oliver_2001_Allergy_56_1087
PubMedSearch : Oliver_2001_Allergy_56_1087
PubMedID: 11703224

Title : Concurrent administration of donepezil HCl and theophylline: assessment of pharmacokinetic changes following multiple-dose administration in healthy volunteers - Tiseo_1998_Br.J.Clin.Pharmacol_46 Suppl 1_35
Author(s) : Tiseo PJ , Foley K , Friedhoff LT
Ref : British Journal of Clinical Pharmacology , 46 Suppl 1 :35 , 1998
Abstract : Tiseo_1998_Br.J.Clin.Pharmacol_46 Suppl 1_35
ESTHER : Tiseo_1998_Br.J.Clin.Pharmacol_46 Suppl 1_35
PubMedSearch : Tiseo_1998_Br.J.Clin.Pharmacol_46 Suppl 1_35
PubMedID: 9839764

Title : Effect of theophylline on airway responses to inhaled platelet-activating factor in man - Chung_1989_Eur.Respir.J_2_763
Author(s) : Chung KF , Lammers JW , McCusker M , Roberts NM , Nichol GM , Barnes PJ
Ref : Eur Respir J , 2 :763 , 1989
Abstract : Chung_1989_Eur.Respir.J_2_763
ESTHER : Chung_1989_Eur.Respir.J_2_763
PubMedSearch : Chung_1989_Eur.Respir.J_2_763
PubMedID: 2680584

Title : Protective effect of oral oxyphenonium bromide, terbutaline and theophylline against the bronchial obstructive effects of inhaled histamine, acetylcholine and propranolol - Koeter_1984_Eur.J.Clin.Pharmacol_26_435
Author(s) : Koeter GH , Meurs H , Jonkman JH , Greving J , Leferink J , Sluiter HJ , de Zeeuw RA , de Vries K
Ref : European Journal of Clinical Pharmacology , 26 :435 , 1984
Abstract : Koeter_1984_Eur.J.Clin.Pharmacol_26_435
ESTHER : Koeter_1984_Eur.J.Clin.Pharmacol_26_435
PubMedSearch : Koeter_1984_Eur.J.Clin.Pharmacol_26_435
PubMedID: 6329769

Title : The time course of changes in cyclic nucleotide levels during cholinergic inhibition of positive inotropic actions of isoprenaline and theophylline in the isolated canine ventricular myocardium -
Author(s) : Endoh M
Ref : Naunyn Schmiedebergs Arch Pharmacol , 312 :175 , 1980
PubMedID: 6250085

Title : Correlation of cyclic AMP and cyclic GMP levels with changes in contractile force of dog ventricular myocardium during cholinergic antagonism of positive inotropic actions of histamine, glucagon, theophylline and papaverine - Endoh_1979_Jpn.J.Pharmacol_29_855
Author(s) : Endoh M
Ref : Japanese Journal of Pharmacology , 29 :855 , 1979
Abstract : Endoh_1979_Jpn.J.Pharmacol_29_855
ESTHER : Endoh_1979_Jpn.J.Pharmacol_29_855
PubMedSearch : Endoh_1979_Jpn.J.Pharmacol_29_855
PubMedID: 232199

Title : Postsynaptic facilitatory effects of theophylline on amphibian neuromyal transmission - Kaibara_1978_J.Pharmacol.Exp.Ther_206_670
Author(s) : Kaibara K , Karczmar AG
Ref : Journal of Pharmacology & Experimental Therapeutics , 206 :670 , 1978
Abstract : Kaibara_1978_J.Pharmacol.Exp.Ther_206_670
ESTHER : Kaibara_1978_J.Pharmacol.Exp.Ther_206_670
PubMedSearch : Kaibara_1978_J.Pharmacol.Exp.Ther_206_670
PubMedID: 212547

Title : A comparison of the effect of theophylline and cyclic adenosine 3': 5'-monophosphate on the superior cervical ganglion of the rabbit by means of the sucrose-gap method -
Author(s) : Dun NJ , Karczmar AG
Ref : Journal of Pharmacology & Experimental Therapeutics , 202 :89 , 1977
PubMedID: 195038

Title : Theophylline compounds and myasthenia gravis. II. Clinical report of nine cases -
Author(s) : Brumlik J , Jacobs R , Karczmar AG
Ref : Clinical Pharmacology & Therapeutics , 14 :380 , 1973
PubMedID: 4349121

Title : Theophylline compounds and myasthenia gravis. I. In vitro studies -
Author(s) : Jacobs R , Karczmar AG , Brumlik J
Ref : Clinical Pharmacology & Therapeutics , 14 :374 , 1973
PubMedID: 4698565

Title : Theophylline preparations in the treatment of myasthenia gravis -
Author(s) : Jacobs R , Brumlik J , Karczmar AG
Ref : Trans Am Neurol Assoc , 96 :158 , 1971
PubMedID: 4333996