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PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
1992-6-5
pubmed:abstractText
The effects of the potassium channel activators, cromakalim, BRL 38227 and pinacidil, and the calcium antagonist, verapamil, have been compared against various spasmogens on airway responses in vitro and in vivo in the guinea pig and also in human isolated bronchi. In guinea pig tracheal spirals, potassium channel activators generally had a greater inhibitory effect than verapamil against tone induced by a wide range of spasmogens (spontaneous, 5-hydroxytryptamine, leukotriene D4, prostaglandin E2). The potassium channel activators had very little effect against potassium chloride- and carbachol-induced tone in guinea pig tracheal spirals [e.g., cromakalim (20 microM) induced relaxations of 0.21 +/- 0.03 (relative to an isoprenaline maximum = 1.0, mean +/- S.E.M.) against carbachol, compared to 0.77 +/- 0.03 against histamine]. In vivo, the potassium channel activators prevented histamine and 5-hydroxytryptamine-induced bronchoconstrictions, but had little inhibitory effect against acetylcholine. In contrast, in human bronchi, cromakalim was capable of inducing powerful concentration-dependent relaxations against carbachol-induced tone [cromakalim (20 microM) induced relaxations of 0.77 +/- 0.09 (relative to isoprenaline = 1.0, mean +/- S.E.M.) against carbachol, compared to 0.95 +/- 0.04 against histamine]. In human bronchi, all the inhibitory agents were more potent and more effective, except that verapamil did not have an increased maximum response. We conclude that potassium channel activators should be effective at relaxing contractions induced by a wide range of spasmogens in man.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
May
pubmed:issn
0022-3565
pubmed:author
pubmed:issnType
Print
pubmed:volume
261
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
429-37
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed-meshheading:1578358-Animals, pubmed-meshheading:1578358-Benzopyrans, pubmed-meshheading:1578358-Bronchi, pubmed-meshheading:1578358-Bronchial Spasm, pubmed-meshheading:1578358-Bronchodilator Agents, pubmed-meshheading:1578358-Carbachol, pubmed-meshheading:1578358-Cromakalim, pubmed-meshheading:1578358-Drug Interactions, pubmed-meshheading:1578358-Female, pubmed-meshheading:1578358-Guanidines, pubmed-meshheading:1578358-Guinea Pigs, pubmed-meshheading:1578358-Humans, pubmed-meshheading:1578358-Male, pubmed-meshheading:1578358-Muscle Contraction, pubmed-meshheading:1578358-Pinacidil, pubmed-meshheading:1578358-Potassium Channels, pubmed-meshheading:1578358-Pyrroles, pubmed-meshheading:1578358-Stereoisomerism, pubmed-meshheading:1578358-Trachea, pubmed-meshheading:1578358-Vasodilator Agents, pubmed-meshheading:1578358-Verapamil
pubmed:year
1992
pubmed:articleTitle
The inhibitory effects of cromakalim and its active enantiomer BRL 38227 against various agonists in guinea pig and human airways: comparison with pinacidil and verapamil.
pubmed:affiliation
SmithKline Beecham Pharmaceuticals, Biosciences Research Centre, Epsom, Surrey, England.
pubmed:publicationType
Journal Article, Comparative Study