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Article: Effects of the methyl xanthine S 9795 on isolated bronchi of the dog

TitleEffects of the methyl xanthine S 9795 on isolated bronchi of the dog
Authors
Issue Date1990
PublisherAmerican Society for Pharmacology and Experimental Therapeutics. The Journal's web site is located at http://jpet.aspetjournals.org
Citation
Journal Of Pharmacology And Experimental Therapeutics, 1990, v. 254 n. 3, p. 1045-1053 How to Cite?
AbstractThe xanthine derivative 1-methyl 3-isobutyl 8-{2-ethyl[1-(4-diphenylmethyl piperazinyl)]}3, 7-dihydro (1H) purine 2, 6-dione (S 9795) is a potent inhibitor of bronchoconstriction in vivo. The aim of the present study was to analyze the effects of S 9795 in vitro and determine whether S 9795 affects the autonomic nerves, the epithelium or the smooth muscle of the bronchial wall. S 9795 had an inhibitory effect on the contractile responses evoked by acetylcholine and by electrical stimulation of the cholinergic nerves. S 9795 appeared more potent against contractions evoked by nerve stimulation. In addition, S 9795 caused the release of [ 3H]norepinephrine from the adrenergic nerve endings but did not affect neuronal uptake of the catecholamine. At low concentrations, S 9795 acted as a competitive serotonergic antagonist; at higher concentrations, the compound inhibited noncompetitively the contractions evoked by histamine and acetylcholine. In both second and fourth order bronchi, S 9795 (and theophylline) produced concentration-dependent relaxations that were significantly greater in rings with, compared with rings without, epithelium. The compound also facilitated the epithelium-dependent component of the relaxation response to beta-adrenergic activation. These results suggest that S 9795: 1) causes prejunctional inhibition of the release of acetylcholine, 2) evokes the displacement of stored norepinephrine, 3) exerts a differential inhibitory effect on airway contractions induced by various bronchoconstrictors and 4) augments the release or facilitates the effect of the epithelium-derived relaxing factor. These effects could contribute to the bronchodilator effect of the drug.
Persistent Identifierhttp://hdl.handle.net/10722/170969
ISSN
2015 Impact Factor: 3.76
2015 SCImago Journal Rankings: 1.847
ISI Accession Number ID

 

DC FieldValueLanguage
dc.contributor.authorBusk, MFen_US
dc.contributor.authorFlavahan, NAen_US
dc.contributor.authorVanhoutte, PMen_US
dc.date.accessioned2012-10-30T06:11:39Z-
dc.date.available2012-10-30T06:11:39Z-
dc.date.issued1990en_US
dc.identifier.citationJournal Of Pharmacology And Experimental Therapeutics, 1990, v. 254 n. 3, p. 1045-1053en_US
dc.identifier.issn0022-3565en_US
dc.identifier.urihttp://hdl.handle.net/10722/170969-
dc.description.abstractThe xanthine derivative 1-methyl 3-isobutyl 8-{2-ethyl[1-(4-diphenylmethyl piperazinyl)]}3, 7-dihydro (1H) purine 2, 6-dione (S 9795) is a potent inhibitor of bronchoconstriction in vivo. The aim of the present study was to analyze the effects of S 9795 in vitro and determine whether S 9795 affects the autonomic nerves, the epithelium or the smooth muscle of the bronchial wall. S 9795 had an inhibitory effect on the contractile responses evoked by acetylcholine and by electrical stimulation of the cholinergic nerves. S 9795 appeared more potent against contractions evoked by nerve stimulation. In addition, S 9795 caused the release of [ 3H]norepinephrine from the adrenergic nerve endings but did not affect neuronal uptake of the catecholamine. At low concentrations, S 9795 acted as a competitive serotonergic antagonist; at higher concentrations, the compound inhibited noncompetitively the contractions evoked by histamine and acetylcholine. In both second and fourth order bronchi, S 9795 (and theophylline) produced concentration-dependent relaxations that were significantly greater in rings with, compared with rings without, epithelium. The compound also facilitated the epithelium-dependent component of the relaxation response to beta-adrenergic activation. These results suggest that S 9795: 1) causes prejunctional inhibition of the release of acetylcholine, 2) evokes the displacement of stored norepinephrine, 3) exerts a differential inhibitory effect on airway contractions induced by various bronchoconstrictors and 4) augments the release or facilitates the effect of the epithelium-derived relaxing factor. These effects could contribute to the bronchodilator effect of the drug.en_US
dc.languageengen_US
dc.publisherAmerican Society for Pharmacology and Experimental Therapeutics. The Journal's web site is located at http://jpet.aspetjournals.orgen_US
dc.relation.ispartofJournal of Pharmacology and Experimental Therapeuticsen_US
dc.subject.meshAcetylcholine - Pharmacologyen_US
dc.subject.meshAnimalsen_US
dc.subject.meshBronchi - Drug Effects - Metabolismen_US
dc.subject.meshBronchodilator Agents - Pharmacologyen_US
dc.subject.meshCulture Techniquesen_US
dc.subject.meshDogsen_US
dc.subject.meshElectric Stimulationen_US
dc.subject.meshFemaleen_US
dc.subject.meshMaleen_US
dc.subject.meshNerve Endings - Drug Effectsen_US
dc.subject.meshNitric Oxide - Metabolismen_US
dc.subject.meshNorepinephrine - Metabolismen_US
dc.subject.meshXanthines - Pharmacologyen_US
dc.titleEffects of the methyl xanthine S 9795 on isolated bronchi of the dogen_US
dc.typeArticleen_US
dc.identifier.emailVanhoutte, PM:vanhoutt@hku.hken_US
dc.identifier.authorityVanhoutte, PM=rp00238en_US
dc.description.naturelink_to_subscribed_fulltexten_US
dc.identifier.pmid2395105-
dc.identifier.scopuseid_2-s2.0-0024997613en_US
dc.identifier.volume254en_US
dc.identifier.issue3en_US
dc.identifier.spage1045en_US
dc.identifier.epage1053en_US
dc.identifier.isiWOS:A1990DY62000042-
dc.publisher.placeUnited Statesen_US
dc.identifier.scopusauthoridBusk, MF=6602700453en_US
dc.identifier.scopusauthoridFlavahan, NA=7006398882en_US
dc.identifier.scopusauthoridVanhoutte, PM=7202304247en_US

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