Biomaterial Database

Inhibitory effect of theophylline, theophylline-7-acetic acid, ambroxol and ambroxol-theophylline-7-acetate on rat lung cAMP phosphodiesterase isoenzymes. 1992

C Ferretti, and G Coppi, and M Blengio, and E Genazzani

Institute of Pharmacology and Experimental Therapy, University of Turin, Italy.

It is assumed that theophylline (THEO) and its xanthinic derivatives inhibit lung phosphodiesterase (PDE) and block adenosine receptors in the induction of bronchodilatation. Since the theophyllinic compound ambroxol-theophylline-7-acetic acid (ATA) has been shown in vivo to be a sound bronchodilator, this paper compares the action of ambroxol-theophylline-7-acetate (ATA), its two components, theophylline-7-acetic acid (TAA) and ambroxol (AMB), and theophylline (THEO) on the hydrolytic activity of three rat-lung cAMP PDE (types I, III and IV) and on striatal adenosine receptors. THEO inhibited all three isoenzymes with equal intensity, whereas ATA was as powerful but inhibited types III and IV only, on which AMB and TAA also showed lower effects. Lastly, unlike THEO, ATA and its two components were unable to antagonize adenosine receptors. Taken as a whole, these results suggest that the bronchodilating activity of ATA is the result of specific inhibition of particular forms of PDE and is thus more specific than that of THEO alone.

UI	MeSH Term	Description	Entries
D007527	Isoenzymes	Structurally related forms of an enzyme. Each isoenzyme has the same mechanism and classification, but differs in its chemical, physical, or immunological characteristics.	Alloenzyme,Allozyme,Isoenzyme,Isozyme,Isozymes,Alloenzymes,Allozymes
D008168	Lung	Either of the pair of organs occupying the cavity of the thorax that effect the aeration of the blood.	Lungs
D008297	Male		Males
D011869	Radioligand Assay	Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).	Protein-Binding Radioassay,Radioreceptor Assay,Assay, Radioligand,Assay, Radioreceptor,Assays, Radioligand,Assays, Radioreceptor,Protein Binding Radioassay,Protein-Binding Radioassays,Radioassay, Protein-Binding,Radioassays, Protein-Binding,Radioligand Assays,Radioreceptor Assays
D011983	Receptors, Purinergic	Cell surface proteins that bind PURINES with high affinity and trigger intracellular changes which influence the behavior of cells. The best characterized classes of purinergic receptors in mammals are the P1 receptors, which prefer ADENOSINE, and the P2 receptors, which prefer ATP or ADP.	Methyladenine Receptors,Purine Receptors,Purinergic Receptor,Purinergic Receptors,Purinoceptors,Purine Receptor,Purinoceptor,Receptors, Methyladenine,Receptors, Purine,Receptor, Purine,Receptor, Purinergic
D001993	Bronchodilator Agents	Agents that cause an increase in the expansion of a bronchus or bronchial tubes.	Bronchial-Dilating Agents,Bronchodilator,Bronchodilator Agent,Broncholytic Agent,Bronchodilator Effect,Bronchodilator Effects,Bronchodilators,Broncholytic Agents,Broncholytic Effect,Broncholytic Effects,Agent, Bronchodilator,Agent, Broncholytic,Agents, Bronchial-Dilating,Agents, Bronchodilator,Agents, Broncholytic,Bronchial Dilating Agents,Effect, Bronchodilator,Effect, Broncholytic,Effects, Bronchodilator,Effects, Broncholytic
D000551	Ambroxol	A metabolite of BROMHEXINE that stimulates mucociliary action and clears the air passages in the respiratory tract. It is usually administered as the hydrochloride.	Bromhexine Metabolite VIII,4-(((2-Amino-3,5-dibromophenyl)methyl)amino)cyclohexanol,AMBROPP,Abrohexal,Ambril,Ambro-Puren,Ambrobeta,Ambrofur,Ambrohexal,Ambrolitic,Ambrolös,Ambroten,Ambroxin,Ambroxocompren,Bisolvon AM,Bronchopront,Bronchowern,Broxol,Contac Husten-Trunk,Dinobroxol,Duramucal,Ebromin,Expeflen,Expit,Farmabroxol,Flavamed,Frenopect,Gelopol,Larylin Husten-Löser,Lasolvan,Mibrox,Motosol,Muco-Fips,Mucosolvan,Mucotablin,NA-872,Pect Hustenlöser,Pulmonal S,Pädiamuc,Ringelheimer Pulmonal,Sekretovit,Surbronc,Therapin Hustenlöser,stas-Hustenlöser,AM, Bisolvon,Ambro Puren,AmbroPuren,Contac Husten Trunk,Contac HustenTrunk,Hustenlöser, Pect,Hustenlöser, Therapin,Larylin Husten Löser,Larylin HustenLöser,Metabolite VIII, Bromhexine,Muco Fips,MucoFips,NA 872,NA872,Pulmonal, Ringelheimer,stas Hustenlöser,stasHustenlöser
D000818	Animals	Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA.	Animal,Metazoa,Animalia
D013806	Theophylline	A methyl xanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac and central nervous system stimulant activities. Theophylline inhibits the 3',5'-CYCLIC NUCLEOTIDE PHOSPHODIESTERASE that degrades CYCLIC AMP thus potentiates the actions of agents that act through ADENYLYL CYCLASES and cyclic AMP.	1,3-Dimethylxanthine,3,7-Dihydro-1,3-dimethyl-1H-purine-2,6-dione,Accurbron,Aerobin,Aerolate,Afonilum Retard,Aquaphyllin,Armophylline,Bronchoparat,Bronkodyl,Constant-T,Elixophyllin,Euphylong,Glycine Theophyllinate,Lodrane,Monospan,Nuelin,Nuelin S.A.,Quibron T-SR,Slo-Phyllin,Somophyllin-T,Sustaire,Synophylate,Theo Von Ct,Theo-24,Theo-Dur,Theobid,Theocin,Theoconfin Continuous,Theodur,Theolair,Theolix,Theon,Theonite,Theopek,Theophylline Anhydrous,Theophylline Sodium Glycinate,Theospan,Theostat,Theovent,Uniphyl,Uniphyllin,Uniphylline,1,3 Dimethylxanthine,Anhydrous, Theophylline,Constant T,ConstantT,Ct, Theo Von,Glycinate, Theophylline Sodium,Quibron T SR,Quibron TSR,Slo Phyllin,SloPhyllin,Sodium Glycinate, Theophylline,Somophyllin T,SomophyllinT,Theo 24,Theo Dur,Theo24,Theophyllinate, Glycine,Von Ct, Theo
D014970	Xanthines	Purine bases found in body tissues and fluids and in some plants.