Source:http://linkedlifedata.com/resource/pubmed/id/10374714
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
1
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| pubmed:dateCreated |
1999-7-21
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| pubmed:abstractText |
5-Hydroxytryptamine (5-HT) can produce both vasoconstrictor and vasorelaxant effects in human coronary arteries and the response to 5-HT can be influenced by the presence of disease. The aim of the present study was to elucidate the 5-HT receptor subtypes responsible for mediating 5-HT-evoked contraction of human coronary arteries using pharmacological, molecular and immunocytochemical approaches. Normal human coronary arteries, with intact endothelium, were mounted in tissue baths, and the vascular responses to 5-HT and 5-HT receptor agonists were studied. The effects of 5-HT1 and 5-HT2 receptor antagonists on these responses were also studied. Expression of messenger ribonucleic acid (mRNA) encoding different 5-HT receptors in human coronary arteries, atrium, ventricle wall and epicardium was determined using reverse transcriptase-polymerase chain reaction (RT-PCR) and Southern blot analysis. The expression of 5-HT1B or 5-HT1D receptor protein was studied using subtype selective antibodies and standard immunocytochemical techniques. The rank order of 5-HT receptor agonist potency in causing vasoconstriction was 5-carboxamido tryptamine, (5-CT) > zolmitriptan = BW183C91 (N10-desmethyl zolmitriptan) = alpha-methyl-5-hydroxytryptamine (alpha-CH3-5-HT) = 5-HT = sumatriptan > 2-methyl-5-hydroxytryptamine (2-CH3-5-HT) = 8-hydroxy-DPAT (8-OH-DPAT). Alpha-CH3-5-HT, 5-CT, 5-HT, zolmitriptan and BW 183C91 were significantly more potent (approximately 3-fold) than sumatriptan and 2-CH3-5-HT, which in turn were more potent than 8-OH-DPAT. Ketanserin and methiothepin (5-HT2 and 5-HT1 receptor antagonists, respectively) caused parallel rightward shifts of the concentration-effect curves to alpha-CH3-5-HT or 5-CT, respectively, without changing the maximum contractile response. In human coronary arteries, atrium. ventricle and epicardium. RT-PCR products corresponding to the human 5-HT2A, 5-HT1B and 5-HT1F receptors were expressed in high levels, mRNAs coding for 5-HT7, 5-HT1A and 5-HT1D receptors were only weakly expressed. No 5-HT1F receptor mRNA was detected. In coronary arteries there was a differential expression of 5-HT1B versus 5-HT1D receptor mRNAs, with 5-HT1B mRNAs being found in greater abundance. Dense 5-HT1B-immunoreactivity was detected on smooth muscle layer within coronary artery, however, 5-HT1D-immunoreactivity was not detected. It is concluded that 5-HT-evoked contraction of human coronary arteries is most probably mediated via the activation of both 5-HT1B and 5-HT2A 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/2-methyl-5-HT,
http://linkedlifedata.com/resource/pubmed/chemical/5-carboxamidotryptamine,
http://linkedlifedata.com/resource/pubmed/chemical/8-Hydroxy-2-(di-n-propylamino)tetral...,
http://linkedlifedata.com/resource/pubmed/chemical/HTR1B protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Ketanserin,
http://linkedlifedata.com/resource/pubmed/chemical/Methiothepin,
http://linkedlifedata.com/resource/pubmed/chemical/Oxazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Oxazolidinones,
http://linkedlifedata.com/resource/pubmed/chemical/RNA, Messenger,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Serotonin, 5-HT1B,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Serotonin, 5-HT1D,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin Receptor Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/Sumatriptan,
http://linkedlifedata.com/resource/pubmed/chemical/Tryptamines,
http://linkedlifedata.com/resource/pubmed/chemical/zolmitriptan
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| pubmed:status |
MEDLINE
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| pubmed:month |
May
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| pubmed:issn |
0014-2999
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| pubmed:author | |
| pubmed:issnType |
Print
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| pubmed:day |
7
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| pubmed:volume |
372
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| pubmed:owner |
NLM
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| pubmed:authorsComplete |
Y
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| pubmed:pagination |
49-56
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| pubmed:dateRevised |
2010-11-18
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| pubmed:meshHeading |
pubmed-meshheading:10374714-8-Hydroxy-2-(di-n-propylamino)tetralin,
pubmed-meshheading:10374714-Cardiovascular System,
pubmed-meshheading:10374714-Coronary Vessels,
pubmed-meshheading:10374714-Dose-Response Relationship, Drug,
pubmed-meshheading:10374714-Gene Expression,
pubmed-meshheading:10374714-Humans,
pubmed-meshheading:10374714-Immunohistochemistry,
pubmed-meshheading:10374714-Ketanserin,
pubmed-meshheading:10374714-Methiothepin,
pubmed-meshheading:10374714-Oxazoles,
pubmed-meshheading:10374714-Oxazolidinones,
pubmed-meshheading:10374714-RNA, Messenger,
pubmed-meshheading:10374714-Receptor, Serotonin, 5-HT1B,
pubmed-meshheading:10374714-Receptor, Serotonin, 5-HT1D,
pubmed-meshheading:10374714-Receptors, Serotonin,
pubmed-meshheading:10374714-Reverse Transcriptase Polymerase Chain Reaction,
pubmed-meshheading:10374714-Serotonin,
pubmed-meshheading:10374714-Serotonin Antagonists,
pubmed-meshheading:10374714-Serotonin Receptor Agonists,
pubmed-meshheading:10374714-Sumatriptan,
pubmed-meshheading:10374714-Tissue Distribution,
pubmed-meshheading:10374714-Tryptamines,
pubmed-meshheading:10374714-Vasoconstriction
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| pubmed:year |
1999
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| pubmed:articleTitle |
Characterisation of 5-HT receptors in human coronary arteries by molecular and pharmacological techniques.
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| pubmed:affiliation |
Department of Internal Medicine, Lund University Hospital, Sweden.
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| pubmed:publicationType |
Journal Article,
Comparative Study,
In Vitro,
Research Support, Non-U.S. Gov't
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