pubmed-article:3207991 | rdf:type | pubmed:Citation | lld:pubmed |
pubmed-article:3207991 | lifeskim:mentions | umls-concept:C0999699 | lld:lifeskim |
pubmed-article:3207991 | lifeskim:mentions | umls-concept:C0006280 | lld:lifeskim |
pubmed-article:3207991 | lifeskim:mentions | umls-concept:C0028066 | lld:lifeskim |
pubmed-article:3207991 | lifeskim:mentions | umls-concept:C0032824 | lld:lifeskim |
pubmed-article:3207991 | lifeskim:mentions | umls-concept:C0056506 | lld:lifeskim |
pubmed-article:3207991 | lifeskim:mentions | umls-concept:C1412820 | lld:lifeskim |
pubmed-article:3207991 | lifeskim:mentions | umls-concept:C0220825 | lld:lifeskim |
pubmed-article:3207991 | lifeskim:mentions | umls-concept:C1707455 | lld:lifeskim |
pubmed-article:3207991 | pubmed:issue | 3 | lld:pubmed |
pubmed-article:3207991 | pubmed:dateCreated | 1989-2-16 | lld:pubmed |
pubmed-article:3207991 | pubmed:abstractText | 1. The potential of the potassium channel activator, cromakalim (BRL 34915), as a bronchodilator has been evaluated in guinea-pig models in comparison with nifedipine. Some effects of the compounds on guinea-pig tracheal spirals have been studied in an attempt to elucidate their different efficacies in vivo. 2. When given by the intraduodenal route to anaesthetized guinea-pigs, cromakalim (3 and 10 mg kg-1) inhibited 5-hydroxytryptamine (5-HT)-induced bronchospasm for at least 60 min. When given by the i.v. route, the dose of cromakalim producing 50% inhibition of the 5-HT response was 84 micrograms kg-1. Nifedipine failed to show any protective effect up to 100 micrograms kg-1, i.v. and was lethal at higher dose levels. 3. Cromakalim protected conscious guinea-pigs from asphyxic collapse in response to histamine aerosol. The maximal effect occurred 60 min following oral dosing, with 2.5 mg kg-1 providing complete protection for almost half of the animals. Nifedipine had only a weak protective effect even at a high dose level of 50 mg kg-1, p.o. 4. Cromakalim prolonged the time before convulsive cough in response to an antigen challenge in actively sensitized guinea-pigs. Its minimum protective dose was 1 mg kg-1, p.o. Nifedipine (50 mg kg-1, p.o.) was ineffective. 5. Cromakalim inhibited both spontaneous and prostaglandin E2-induced tone in guinea-pig isolated tracheal spirals with IC50 values, relative to the maximum inhibition achieved by isoprenaline (10(-3)M), of 1.1 x 10(-6)M and 8.9 x 10(-7)M, respectively. Its maximal effect was 89% of that produced by isoprenaline. Removal of the epithelium did not influence its activity. Studies using the two enantiomers showed that the activity of cromakalim resided almost entirely in the (-)-enantiomer. 6. Nifedipine (2 x 10-SM) achieved only 49% of the relaxant effect of 10 -3M isoprenaline in isolated tracheal spirals. Addition of cromakalim (10- 5 M) at the end of the nifedipine concentrationresponse experiment caused further relaxation to 94% of the effect of isoprenaline. 7. It is concluded that cromakalim has greater potential than nifedipine as a bronchodilator. It appears that opening of potassium channels, with consequent hyperpolarization and stabilization of the membrane potential, prevents calcium entering the cytosol through routes that are unaffected by calcium entry blockers. | lld:pubmed |
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pubmed-article:3207991 | pubmed:language | eng | lld:pubmed |
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pubmed-article:3207991 | pubmed:citationSubset | IM | lld:pubmed |
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pubmed-article:3207991 | pubmed:status | MEDLINE | lld:pubmed |
pubmed-article:3207991 | pubmed:month | Nov | lld:pubmed |
pubmed-article:3207991 | pubmed:issn | 0007-1188 | lld:pubmed |
pubmed-article:3207991 | pubmed:author | pubmed-author:TaylorJ FJF | lld:pubmed |
pubmed-article:3207991 | pubmed:author | pubmed-author:BuckleD RDR | lld:pubmed |
pubmed-article:3207991 | pubmed:author | pubmed-author:TaylorS GSG | lld:pubmed |
pubmed-article:3207991 | pubmed:author | pubmed-author:ArchJ RJR | lld:pubmed |
pubmed-article:3207991 | pubmed:author | pubmed-author:ClarkeG DGD | lld:pubmed |
pubmed-article:3207991 | pubmed:author | pubmed-author:BumsteadJJ | lld:pubmed |
pubmed-article:3207991 | pubmed:issnType | Print | lld:pubmed |
pubmed-article:3207991 | pubmed:volume | 95 | lld:pubmed |
pubmed-article:3207991 | pubmed:owner | NLM | lld:pubmed |
pubmed-article:3207991 | pubmed:authorsComplete | Y | lld:pubmed |
pubmed-article:3207991 | pubmed:pagination | 763-70 | lld:pubmed |
pubmed-article:3207991 | pubmed:dateRevised | 2010-4-19 | lld:pubmed |
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pubmed-article:3207991 | pubmed:year | 1988 | lld:pubmed |
pubmed-article:3207991 | pubmed:articleTitle | Evaluation of the potassium channel activator cromakalim (BRL 34915) as a bronchodilator in the guinea-pig: comparison with nifedipine. | lld:pubmed |
pubmed-article:3207991 | pubmed:affiliation | Beecham Pharmaceuticals Research Division, Biosciences Research Centre, Epsom, Surrey. | lld:pubmed |
pubmed-article:3207991 | pubmed:publicationType | Journal Article | lld:pubmed |
pubmed-article:3207991 | pubmed:publicationType | Comparative Study | lld:pubmed |
pubmed-article:3207991 | pubmed:publicationType | In Vitro | lld:pubmed |
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