| The effect of the selective PAF antagonist CIS-19 on PAF- and antigen-induced bronchoconstriction, microvascular leakage and bronchial hyperreactivity in guinea-pigs. | |
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MedLine Citation:
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PMID: 9050014 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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We investigated the effects of a novel platelet-activating factor (PAF) receptor antagonist, CIS-19 [cis-2-(3, 4-dimethoxyphenyl)-6-isopropoxy-7-methoxy-1-(N-methyl-formamido)-1, 2, 3, 4-tetrahydronaphthalene], on PAF-, histamine-, substance P- and antigen-induced bronchoconstriction and microvascular leakage, as well as PAF- and antigen-induced bronchial hyperreactivity to methacholine in urethane-anesthetized guinea-pigs. Administration of CIS-19 (0.5-5 mg/kg, i.v.) inhibited the increase in lung resistance induced by PAF (30 ng/kg, i.v.) in a dose-dependent manner, but failed to inhibit the increase induced by histamine (30 micrograms/kg, i.v.) or substance P (6.5 micrograms/kg, i.v.). CIS-19 (5 mg/kg, i.v.) did not inhibit the increase in lung resistance induced by ovalbumin (2 mg/kg, i.v.) in actively sensitized guinea-pigs. PAF (30 ng/kg, i.v.)-induced microvascular leakage, measured by the extravasation of Evans blue dye, was dose-dependently inhibited by CIS-19 (0.5-5 mg/kg, i.v.) in the trachea, main bronchi and intrapulmonary airways, but it did not affect histamine (30 micrograms/kg, i.v.)- or substance P (6.5 micrograms/kg, i.v.)-induced microvascular leakage at all airway levels. CIS-19 (2.5 and 5 mg/kg) did not affect ovalbumin (2 mg/kg, i.v.)-induced microvascular leakage in all airway levels in actively sensitized guinea-pigs, CIS-19 (2.5 and 5 mg/kg, i.v.) significantly inhibited PAF-induced enhancement of the bronchial response to methacholine, but had no effect on ovalbumin (0.05 mg/kg, i.v.)-induced bronchial hyperreactivity in actively sensitized guinea-pigs. It is concluded that CIS-19 is a potent PAF receptor antagonist which inhibits PAF- but not antigen-induced bronchoconstriction, microvascular leakage and bronchial hyperreactivity. These results suggest that PAF plays little or no role in early airway responses following antigen challenge. |
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Authors:
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C H Lin; F N Ko; H Ishii; T Ishikawa; I S Chen; C M Teng; H P Kuo |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Naunyn-Schmiedeberg's archives of pharmacology Volume: 355 ISSN: 0028-1298 ISO Abbreviation: Naunyn Schmiedebergs Arch. Pharmacol. Publication Date: 1997 Feb |
Date Detail:
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Created Date: 1997-05-27 Completed Date: 1997-05-27 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 0326264 Medline TA: Naunyn Schmiedebergs Arch Pharmacol Country: GERMANY |
Other Details:
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Languages: eng Pagination: 210-6 Citation Subset: IM |
Affiliation:
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Pharmacological Institute, College of Medicine, National Taiwan University, Taipei. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Airway Resistance
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drug effects Animals Antigens / immunology Bronchoconstriction / drug effects*, immunology Bronchoconstrictor Agents / pharmacology Capillary Permeability / drug effects* Guinea Pigs Histamine / pharmacology Male Methacholine Chloride / pharmacology Platelet Activating Factor / toxicity Platelet Membrane Glycoproteins / antagonists & inhibitors* Rats Receptors, Cell Surface* Receptors, G-Protein-Coupled* Respiratory Hypersensitivity / chemically induced, immunology, prevention & control* Substance P / pharmacology Tetrahydronaphthalenes / pharmacology* |
| Chemical | |
Reg. No./Substance:
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0/Antigens; 0/Bronchoconstrictor Agents; 0/Platelet Activating Factor; 0/Platelet Membrane Glycoproteins; 0/Receptors, Cell Surface; 0/Receptors, G-Protein-Coupled; 0/Tetrahydronaphthalenes; 0/platelet activating factor receptor; 33507-63-0/Substance P; 51-45-6/Histamine; 62-51-1/Methacholine Chloride; 88114-56-1/CIS 19 |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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