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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
7
|
| pubmed:dateCreated |
1998-11-13
|
| pubmed:abstractText |
1. In the human temporal artery both 5-HT1-like and 5-HT2A receptors mediate the contractile effects of 5-hydroxytryptamine (5-HT) and we have suggested that the 5-HT1-like receptors resemble more closely recombinant 5-HT1B than 5-HT1D receptors. To investigate further which subtype is involved, we investigated the blockade of 5-HT-induced contractions by the 5-HT1B-selective antagonist SB-224289 (2,3,6,7-tetrahydro-1'-methyl-5-[2-methyl-4'[(5-methyl-1,2,4-oxadiazole- 3-yl) biphenyl-4-yl] carbonyl] furo[2,3-f]indole-3-spiro-4'-piperidine oxalate) and the 5-HT1D-selective antagonist BRL-15572 (1-phenyl-3[4-3-chlorophenyl piperazin-1-yl] phenylpropan-2-ol). We also used RT-PCR to search for the mRNA of 5-HT1B, 5-HT1D and other 5-HT receptors. 2. The contractile effects of 5-HT in temporal artery rings were partially antagonized by SB-224289 (20, 200 nM) (apparent KB = 1 nM) and ketanserin (1 microM) but not by BRL-15572 (500 nM). 3. Sumatriptan evoked contractions (EC50, 170 nM) that were resistant to blockade by BRL-15572 (500 nM) but antagonized by SB-224289 (20, 200 nM). 4. The potency of 5-HT (EC50) was estimated to be 94 nM for the ketanserin-sensitive receptor and 34 nM for the SB-224289-sensitive receptor. The fraction of maximal 5-HT response mediated through SB-224289-sensitive receptors was 0.20-0.67, the remainder being mediated through ketanserin-sensitive receptors. 5. We detected arterial receptor mRNA for the following receptors (incidence): 5-HT1B (8/8), 5-HT1D (2/8), 5-HT1F (0/4), 5-HT2A (0/8) 5-HT2B (0/8), 5-HT2C (0/8), 5-HT4 (4/8) and 5-HT7 (4/8). 6. We conclude that the ketanserin-resistant fraction of the 5-HT effects and the effects of sumatriptan are mediated by 5-HT1B receptors. The lack of antagonism by BRL-15572 rules out 5-HT1D receptors as mediators of the contractile effects of 5-HT and sumatriptan.
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| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/BRL 15572,
http://linkedlifedata.com/resource/pubmed/chemical/Biphenyl Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/DNA Primers,
http://linkedlifedata.com/resource/pubmed/chemical/HTR1B protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Piperazines,
http://linkedlifedata.com/resource/pubmed/chemical/Piperidones,
http://linkedlifedata.com/resource/pubmed/chemical/RNA, Messenger,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Serotonin, 5-HT1B,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/SB 22489G,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Spiro Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/Sumatriptan
|
| pubmed:status |
MEDLINE
|
| pubmed:month |
Aug
|
| pubmed:issn |
0007-1188
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| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:volume |
124
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
1345-54
|
| pubmed:dateRevised |
2008-11-20
|
| pubmed:meshHeading |
pubmed-meshheading:9723944-Adolescent,
pubmed-meshheading:9723944-Adult,
pubmed-meshheading:9723944-Aged,
pubmed-meshheading:9723944-Base Sequence,
pubmed-meshheading:9723944-Biphenyl Compounds,
pubmed-meshheading:9723944-DNA Primers,
pubmed-meshheading:9723944-Female,
pubmed-meshheading:9723944-Humans,
pubmed-meshheading:9723944-Male,
pubmed-meshheading:9723944-Middle Aged,
pubmed-meshheading:9723944-Muscle Contraction,
pubmed-meshheading:9723944-Piperazines,
pubmed-meshheading:9723944-Piperidones,
pubmed-meshheading:9723944-RNA, Messenger,
pubmed-meshheading:9723944-Receptor, Serotonin, 5-HT1B,
pubmed-meshheading:9723944-Receptors, Serotonin,
pubmed-meshheading:9723944-Serotonin Antagonists,
pubmed-meshheading:9723944-Spiro Compounds,
pubmed-meshheading:9723944-Sumatriptan,
pubmed-meshheading:9723944-Temporal Arteries
|
| pubmed:year |
1998
|
| pubmed:articleTitle |
5-HT1B receptor-mediated contractions in human temporal artery: evidence from selective antagonists and 5-HT receptor mRNA expression.
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| pubmed:affiliation |
Department of Neurosurgery, University of Göttingen, Germany.
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| pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't
|