Source:http://linkedlifedata.com/resource/pubmed/id/12489250
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Predicate | Object |
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rdf:type | |
lifeskim:mentions |
umls-concept:C0001492,
umls-concept:C0001644,
umls-concept:C0086376,
umls-concept:C0086418,
umls-concept:C0225595,
umls-concept:C0332282,
umls-concept:C0439851,
umls-concept:C0439852,
umls-concept:C0871261,
umls-concept:C1280500,
umls-concept:C1552596,
umls-concept:C1704632,
umls-concept:C1706817,
umls-concept:C1879547,
umls-concept:C1947931,
umls-concept:C2911692
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pubmed:issue |
11
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pubmed:dateCreated |
2002-12-19
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pubmed:abstractText |
To examine the response to beta-adrenergic receptor agonists (beta-agonists) following prolonged activation of the stimulatory G protein of adenylyl cyclase (Gs), relaxation by isoproterenol (isoprenaline, CAS 949-36-0) and formoterol (CAS 73573-87-2), a long-acting beta-agonist, after exposure to formoterol was measured in human tracheal smooth muscle, using isometric tension records. Prior exposure to formoterol (0.3-30 nmol/l) for 45 min reduced the subsequent relaxation induced by this drug in a concentration-dependent manner, but only modestly reduced that induced by isoproterenol. Next, the effects of cholera toxin (CTX, CAS 9012-63-9) an irreversible direct activator of Gs and formoterol on the reduced responsiveness to isoproterenol after continuous and repeated exposure to isoprotenerol were examined. Preincubation with cholera toxin (0.02-2 micrograms/ml) caused concentration-dependent inhibition of the desensitization induced by isoproterenol, but preincubation with formoterol did not. These results indicate that prolonged activation of Gs via beta-adrenergic receptors does not cause cross-desensitization to short-acting beta-agonists. However, it also fails to inhibit the desensitization of beta-adrenergic receptors after excessive exposure to short-acting beta-agonists. Activation of Gs via a pathway that bypasses the receptors may be beneficial for the prevention of this phenomenon.
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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/Adrenergic beta-Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/Bronchoconstrictor Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Cholera Toxin,
http://linkedlifedata.com/resource/pubmed/chemical/Heterotrimeric GTP-Binding Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Isoproterenol,
http://linkedlifedata.com/resource/pubmed/chemical/Methacholine Chloride
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pubmed:status |
MEDLINE
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pubmed:issn |
0004-4172
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
52
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
803-12
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:12489250-Adrenergic beta-Agonists,
pubmed-meshheading:12489250-Aged,
pubmed-meshheading:12489250-Aged, 80 and over,
pubmed-meshheading:12489250-Bronchoconstrictor Agents,
pubmed-meshheading:12489250-Cholera Toxin,
pubmed-meshheading:12489250-Enzyme Activation,
pubmed-meshheading:12489250-Heterotrimeric GTP-Binding Proteins,
pubmed-meshheading:12489250-Humans,
pubmed-meshheading:12489250-Isoproterenol,
pubmed-meshheading:12489250-Methacholine Chloride,
pubmed-meshheading:12489250-Middle Aged,
pubmed-meshheading:12489250-Muscle, Smooth,
pubmed-meshheading:12489250-Muscle Contraction,
pubmed-meshheading:12489250-Muscle Relaxation,
pubmed-meshheading:12489250-Trachea
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pubmed:year |
2002
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pubmed:articleTitle |
Effects of direct and indirect activation of G protein of adenylyl cyclase on the subsequent response to beta-adrenergic receptor agonists in human trachealis.
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pubmed:affiliation |
Second Department of Internal Medicine, School of Medicine, Nagoya University, Nagoya, Japan.
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pubmed:publicationType |
Journal Article,
In Vitro
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