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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
12
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pubmed:dateCreated |
1994-5-16
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pubmed:abstractText |
We have examined the actions of SR 48968 ((S)-N-methyl-N-[4-(4-acetylamino-4-phenyl piperidino)-2-(3,4-dichlorophenyl)butyl]benzamide), a novel non-peptide tachykinin NK-2-receptor antagonist, on the response evoked by electrical field stimulation or by acetylcholine and neurokinin A on guinea-pig isolated airway smooth muscle. Electrical field stimulation (1-32 Hz, 0.3 ms, 30 V for 20 s) evoked a biphasic response in a frequency-dependent manner, consisting of a cholinergically-mediated fast contraction followed by a non-adrenergically-mediated relaxation in tracheal muscle and by a non-cholinergically-mediated slow contraction in bronchial muscle. SR 48968 (0.01-1 microM) caused a concentration-dependent inhibition of non-cholinergically mediated contraction of bronchial muscle, without significant influence on cholinergically and non-adrenergically-mediated responses. Submaximal contractions of tracheal and bronchial muscles evoked by exogenous neurokinin A (10-300 nM) were markedly inhibited by SR 48968 (0.1-1 microM), but those by exogenous acetylcholine (1-3 microM) were slightly inhibited by the antagonist. The results indicate that in guinea-pig isolated bronchial muscle, SR 48968 selectively inhibited non-cholinergically mediated neurogenic contraction via antagonism of NK-2 receptors.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Acetylcholine,
http://linkedlifedata.com/resource/pubmed/chemical/Benzamides,
http://linkedlifedata.com/resource/pubmed/chemical/Neurokinin A,
http://linkedlifedata.com/resource/pubmed/chemical/Piperidines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Tachykinin,
http://linkedlifedata.com/resource/pubmed/chemical/SR 48968
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pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
0022-3573
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
45
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1037-41
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:7908971-Acetylcholine,
pubmed-meshheading:7908971-Animals,
pubmed-meshheading:7908971-Benzamides,
pubmed-meshheading:7908971-Bronchi,
pubmed-meshheading:7908971-Cholinergic Fibers,
pubmed-meshheading:7908971-Drug Interactions,
pubmed-meshheading:7908971-Electric Stimulation,
pubmed-meshheading:7908971-Guinea Pigs,
pubmed-meshheading:7908971-Male,
pubmed-meshheading:7908971-Muscle, Smooth,
pubmed-meshheading:7908971-Muscle Contraction,
pubmed-meshheading:7908971-Neurokinin A,
pubmed-meshheading:7908971-Piperidines,
pubmed-meshheading:7908971-Receptors, Tachykinin,
pubmed-meshheading:7908971-Trachea
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pubmed:year |
1993
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pubmed:articleTitle |
SR 48968, a novel non-peptide tachykinin NK-2-receptor antagonist, selectively inhibits the non-cholinergically mediated neurogenic contraction of guinea-pig isolated bronchial muscle.
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pubmed:affiliation |
Department of Pharmacology, Dokkyo University School of Medicine, Tochigi, Japan.
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pubmed:publicationType |
Journal Article,
Comparative Study,
In Vitro,
Research Support, Non-U.S. Gov't
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