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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
5 Pt 1
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pubmed:dateCreated |
1997-1-9
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pubmed:abstractText |
On human small isolated bronchi (diameter < 1 mm), but not on larger bronchi (diameter 3-5 mm), substance P (SP) and specific tachykinin SP-preferring neurokinin (NK1) receptor agonists {[beta Ala4, Sar9, Met(O2)11]SP-(4-11), [Sar9, Met(O2)11]SP, [Arg6,Sar9,Met(O2)11]SP-(6-11), and septide; 10(-10) to 10(-6) M} produced a concentration-dependent contraction that occurred at low concentrations (pD2 values of 7.79-8.33) and was characterized by a low intrinsic activity [maximal effect (Emax) of 38-45% of Emax induced by 3 mM acetylcholine, in a noncumulative manner]. Comparison of cumulative and noncumulative concentration-response curves to SP and NK1 receptor agonists suggest rapid receptor desensitization. The SP (10(-8) M)-induced contraction was inhibited by tachykinin NK1 receptor antagonists (rank order of potency: SR-140333 > CP-96,345 > RP-67580) but not by the tachykinin NK2 receptor antagonist SR-48968. Indomethacin (10(-6) M) abolished the SP-induced contraction. Our results suggest that tachykinin NK1 receptors are present on human small bronchi and that their stimulation induces a prostanoid-dependent contraction. The small isolated bronchus is an interesting model of human tissue to test NK1 receptor antagonists.
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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/Benzamides,
http://linkedlifedata.com/resource/pubmed/chemical/Biphenyl Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/CP 96345,
http://linkedlifedata.com/resource/pubmed/chemical/Hormone Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Indomethacin,
http://linkedlifedata.com/resource/pubmed/chemical/Piperidines,
http://linkedlifedata.com/resource/pubmed/chemical/Quinuclidines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Neurokinin-1,
http://linkedlifedata.com/resource/pubmed/chemical/SR 140333,
http://linkedlifedata.com/resource/pubmed/chemical/SR 48968,
http://linkedlifedata.com/resource/pubmed/chemical/Substance P
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
0002-9513
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
271
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
L763-7
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:8944719-Benzamides,
pubmed-meshheading:8944719-Biphenyl Compounds,
pubmed-meshheading:8944719-Bronchi,
pubmed-meshheading:8944719-Female,
pubmed-meshheading:8944719-Hormone Antagonists,
pubmed-meshheading:8944719-Humans,
pubmed-meshheading:8944719-Indomethacin,
pubmed-meshheading:8944719-Lung Neoplasms,
pubmed-meshheading:8944719-Male,
pubmed-meshheading:8944719-Middle Aged,
pubmed-meshheading:8944719-Piperidines,
pubmed-meshheading:8944719-Quinuclidines,
pubmed-meshheading:8944719-Receptors, Neurokinin-1,
pubmed-meshheading:8944719-Substance P
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pubmed:year |
1996
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pubmed:articleTitle |
Evidence for functional tachykinin NK1 receptors on human isolated small bronchi.
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pubmed:affiliation |
Laboratoire de Pharmacologie, Faculté de Médecine Paris Ouest, France.
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pubmed:publicationType |
Journal Article,
In Vitro
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