Biomaterial Database

Interaction of azelastine with adenosine receptors in guinea pig trachea. 1988

U Achterrath-Tuckermann, and I Szelenyi

Department of Pharmacology, Asta Pharma AG, Frankfurt am Main, FRG.

The effects of azelastine, 8-phenyltheophylline, NDGA, atropine and mepyramine on PIA-induced contraction and relaxation of isolated guinea pig tracheal chains were investigated. Atropine (1 nM) and mepyramine (1 microM) had no effect on PIA-induced relaxation whereas 8-phenyltheophylline (5 microM) caused strong inhibition of PIA-induced relaxation, indicating that the latter effect is mediated by stimulation of extracellular adenosine receptors. NDGA (0.5 microM) caused potentiation of PIA-induced relaxation. Azelastine (10 nM-1 microM) caused dose-dependent potentiation of PIA-induced relaxation. In another model for investigation of extracellular adenosine receptors, namely the negative inotropic effect in the electrically driven isolated guinea pig atrium, the action of PIA was fully reversed by the addition of 8-phenyltheophylline. In contrast, the negative inotropic effect of azelastine was not reversed by 8-phenyltheophylline, indicating that azelastine does not act on extracellular adenosine receptors. The negative inotropic effect of azelastine can be reversed by addition of calcium as for verapamil. It is concluded that the calcium-antagonistic and perhaps antiallergic properties of azelastine are responsible for the potentiation of extracellular adenosine receptor mediated relaxation by azelastine. Since asthmatics show increased hyperreagibility (bronchospasm) to inhalation of adenosine, the inhibition of PIA-induced contraction by azelastine indicates that the drug may be worthwhile in the treatment bronchial hyperreactivity in asthmatic patients.

UI	MeSH Term	Description	Entries
D008297	Male		Males
D009126	Muscle Relaxation	That phase of a muscle twitch during which a muscle returns to a resting position.	Muscle Relaxations,Relaxation, Muscle,Relaxations, Muscle
D010660	Phenylisopropyladenosine	N-Isopropyl-N-phenyl-adenosine. Antilipemic agent. Synonym: TH 162.	Isopropylphenyladenosine,L-Phenylisopropyladenosine,N(6)-Phenylisopropyl-Adenosine,L Phenylisopropyladenosine
D010793	Phthalazines	Bicyclic heterocyclic compounds containing a BENZENE ring fused to PYRIDAZINE.
D011724	Pyridazines	Six-membered rings with two adjacent nitrogen atoms also called 1,2-diazine.
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
D006168	Guinea Pigs	A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.	Cavia,Cavia porcellus,Guinea Pig,Pig, Guinea,Pigs, Guinea
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
D014132	Trachea	The cartilaginous and membranous tube descending from the larynx and branching into the right and left main bronchi.	Tracheas