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- Scopus: eid_2-s2.0-0024997613
- PMID: 2395105
- WOS: WOS:A1990DY62000042
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Article: Effects of the methyl xanthine S 9795 on isolated bronchi of the dog
Title | Effects of the methyl xanthine S 9795 on isolated bronchi of the dog |
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Authors | |
Issue Date | 1990 |
Publisher | American 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? |
Abstract | The 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 Identifier | http://hdl.handle.net/10722/170969 |
ISSN | 2023 Impact Factor: 3.1 2023 SCImago Journal Rankings: 0.829 |
ISI Accession Number ID |
DC Field | Value | Language |
---|---|---|
dc.contributor.author | Busk, MF | en_US |
dc.contributor.author | Flavahan, NA | en_US |
dc.contributor.author | Vanhoutte, PM | en_US |
dc.date.accessioned | 2012-10-30T06:11:39Z | - |
dc.date.available | 2012-10-30T06:11:39Z | - |
dc.date.issued | 1990 | en_US |
dc.identifier.citation | Journal Of Pharmacology And Experimental Therapeutics, 1990, v. 254 n. 3, p. 1045-1053 | en_US |
dc.identifier.issn | 0022-3565 | en_US |
dc.identifier.uri | http://hdl.handle.net/10722/170969 | - |
dc.description.abstract | The 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.language | eng | en_US |
dc.publisher | American Society for Pharmacology and Experimental Therapeutics. The Journal's web site is located at http://jpet.aspetjournals.org | en_US |
dc.relation.ispartof | Journal of Pharmacology and Experimental Therapeutics | en_US |
dc.subject.mesh | Acetylcholine - Pharmacology | en_US |
dc.subject.mesh | Animals | en_US |
dc.subject.mesh | Bronchi - Drug Effects - Metabolism | en_US |
dc.subject.mesh | Bronchodilator Agents - Pharmacology | en_US |
dc.subject.mesh | Culture Techniques | en_US |
dc.subject.mesh | Dogs | en_US |
dc.subject.mesh | Electric Stimulation | en_US |
dc.subject.mesh | Female | en_US |
dc.subject.mesh | Male | en_US |
dc.subject.mesh | Nerve Endings - Drug Effects | en_US |
dc.subject.mesh | Nitric Oxide - Metabolism | en_US |
dc.subject.mesh | Norepinephrine - Metabolism | en_US |
dc.subject.mesh | Xanthines - Pharmacology | en_US |
dc.title | Effects of the methyl xanthine S 9795 on isolated bronchi of the dog | en_US |
dc.type | Article | en_US |
dc.identifier.email | Vanhoutte, PM:vanhoutt@hku.hk | en_US |
dc.identifier.authority | Vanhoutte, PM=rp00238 | en_US |
dc.description.nature | link_to_subscribed_fulltext | en_US |
dc.identifier.pmid | 2395105 | - |
dc.identifier.scopus | eid_2-s2.0-0024997613 | en_US |
dc.identifier.volume | 254 | en_US |
dc.identifier.issue | 3 | en_US |
dc.identifier.spage | 1045 | en_US |
dc.identifier.epage | 1053 | en_US |
dc.identifier.isi | WOS:A1990DY62000042 | - |
dc.publisher.place | United States | en_US |
dc.identifier.scopusauthorid | Busk, MF=6602700453 | en_US |
dc.identifier.scopusauthorid | Flavahan, NA=7006398882 | en_US |
dc.identifier.scopusauthorid | Vanhoutte, PM=7202304247 | en_US |
dc.identifier.issnl | 0022-3565 | - |