Source:http://linkedlifedata.com/resource/pubmed/id/12491798
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
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pubmed:dateCreated |
2002-12-20
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pubmed:abstractText |
beta-Adrenoceptor subtypes which mediate relaxation of guinea-pig gastrointestinal smooth muscles in response to catecholamines ((-)-isoprenaline, (-)-noradrenaline and (-)-adrenaline) and beta 3-adrenoceptor agonists (BRL37344 and (+/-)-CGP12177A) are predominantly beta 3-adrenoceptors. Although cAMP-PKA system is thought to play a substantial role in the smooth muscle relaxation mediated via beta 1- and beta 2-adrenoceptors, there is little information on the role of cAMP in beta 3-adrenoceptor-meidated relaxation. The present study was carried out to elucidate the role of cAMP in beta 3-adrenoceptor-meidated relaxation of guinea-pig gastric fundus smooth muscle. Furthermore, possible contribution of two types of K+ (voltage-dependent and Ca(2+)-activated K+, BKCa; voltage-dependent, Kv) channels was also examined pharmaco-mechanically. In gastric fundus smooth muscle, catecholamines and beta 3-adrenoceptor agonists elicited potent relaxations in the presence of beta 1- and beta 2-adrenoceptor antagonists. All of these relaxations were not diminished by an adenylate cyclase inhibitor, SQ-22,536 (100 microM), which indicates their characteristic of cAMP-independency. SQ-22,536-resistant, beta 3-adrenoceptor-mediated relaxations were strongly attenuated by a Kv channel blocker, 4-aminopyridine (3 mM), but not by iberiotoxin (100 nM), a selective blocker of BKCa channel. The present results indicate that 4-aminopyridine-sensitive Kv channels play a primary role in cAMP-independent relaxation of guinea-pig gastric fundus smooth muscle in response to the stimulations of beta 3-adrenoceptors.
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pubmed:language |
jpn
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/4-Aminopyridine,
http://linkedlifedata.com/resource/pubmed/chemical/Adrenergic beta-Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/Catecholamines,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclic AMP,
http://linkedlifedata.com/resource/pubmed/chemical/Potassium Channels, Voltage-Gated,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, beta-3
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
0015-5691
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
120
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
109P-111P
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pubmed:dateRevised |
2011-7-27
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pubmed:meshHeading |
pubmed-meshheading:12491798-4-Aminopyridine,
pubmed-meshheading:12491798-Adrenergic beta-Agonists,
pubmed-meshheading:12491798-Animals,
pubmed-meshheading:12491798-Catecholamines,
pubmed-meshheading:12491798-Cyclic AMP,
pubmed-meshheading:12491798-Gastric Fundus,
pubmed-meshheading:12491798-Guinea Pigs,
pubmed-meshheading:12491798-Male,
pubmed-meshheading:12491798-Muscle, Smooth,
pubmed-meshheading:12491798-Muscle Relaxation,
pubmed-meshheading:12491798-Potassium Channels, Voltage-Gated,
pubmed-meshheading:12491798-Receptors, Adrenergic, beta-3,
pubmed-meshheading:12491798-Signal Transduction
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pubmed:year |
2002
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pubmed:articleTitle |
[Beta 3-adrenoceptor-mediated relaxation of guinea-pig gastric funds smooth muscle: cAMP-independent characteristics and a primary role of 4-aminopyridine-sensitive voltage-dependent K+ (Kv) channels].
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pubmed:affiliation |
Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences, 2-2-1 Miyama, Funabashi-City, Chiba 274-8510, Japan.
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pubmed:publicationType |
Journal Article,
In Vitro,
English Abstract
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