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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
2
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pubmed:dateCreated |
2002-5-15
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pubmed:abstractText |
1. We aimed to characterize 5-HT receptors mediating contraction and relaxation to 5-HT in dog proximal stomach longitudinal muscle (LM) strips. 2. Of the tryptamine analogues tested, 5-HT was the most potent contractile agent at basal length, while 5-CT was the most potent relaxant of PGF(2alpha)-induced contraction. Neither the contractions to 5-HT, nor the relaxations to 5-CT were influenced by tetrodotoxin, illustrating that action potential propagation is not involved. 3. The 5-HT-induced contraction was antagonized by mesulergine (0.03 to 0.3 microM) and ketanserin (2 - 20 nM), but the antagonism was not of a simple competitive nature, indicating multiple receptor involvement. Ketanserin (3 to 30 nM) and mesulergine (30 nM) competitively antagonized the alpha-Me-5-HT-induced contraction (pK(B): 8.83+/-0.09 and pA(2): 8.25+/-0.06 respectively). These affinity values are in line with literature affinities of ketanserin and mesulergine at 5-HT(2A) receptors in various bioassays. 4. The 5-CT-induced inhibition of PGF(2alpha)-induced contraction was competitively antagonized by mesulergine (pK(B) estimate: 8.52+/-0.12) and by the selective 5-HT(7) receptor antagonist SB-269970 (pK(B) estimate: 9.36+/-0.14). Both pK(B) estimates are in line with literature affinities of these compounds for 5-HT(7) receptors. Mesulergine (30 nM) and SB-269970 (10 nM) shifted the relaxant curve to 5-HT parallel to the right in the presence of ketanserin (0.3 microM) (pA(2) estimates of 8.08+/-0.10 and 8.75+/-0.14 respectively), indicative of 5-HT(7) receptor involvement. 5. It is concluded that 5-HT induces dog proximal stomach (LM) contraction via smooth muscle 5-HT(2A) receptors and relaxation via smooth muscle 5-HT(7) receptors.
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/12010782-10082316,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12010782-10556917,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12010782-10669560,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12010782-10716674,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12010782-10807680,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12010782-10821781,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12010782-11230991,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12010782-11309267,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12010782-11704657,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12010782-1451742,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12010782-2540014,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12010782-2866002,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12010782-3416910,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12010782-7506394,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12010782-7602484,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12010782-7938165,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12010782-8012715,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12010782-8032658,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12010782-8223886,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12010782-8226867,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12010782-8380862,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12010782-8566092,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12010782-8894599,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12010782-9051313,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12010782-9300624,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12010782-9430791,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12010782-9950810
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
0007-1188
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
136
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
321-9
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:12010782-Animals,
pubmed-meshheading:12010782-Dogs,
pubmed-meshheading:12010782-Dose-Response Relationship, Drug,
pubmed-meshheading:12010782-Female,
pubmed-meshheading:12010782-Male,
pubmed-meshheading:12010782-Muscle, Smooth,
pubmed-meshheading:12010782-Muscle Contraction,
pubmed-meshheading:12010782-Muscle Relaxation,
pubmed-meshheading:12010782-Receptor, Serotonin, 5-HT2A,
pubmed-meshheading:12010782-Receptors, Serotonin,
pubmed-meshheading:12010782-Serotonin,
pubmed-meshheading:12010782-Serotonin Antagonists,
pubmed-meshheading:12010782-Serotonin Receptor Agonists,
pubmed-meshheading:12010782-Stomach
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pubmed:year |
2002
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pubmed:articleTitle |
Pharmacological characterization of the 5-HT receptors mediating contraction and relaxation of canine isolated proximal stomach smooth muscle.
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pubmed:affiliation |
Heymans Institute of Pharmacology, Ghent University, Gent, Belgium. pjansse42@janbe.jnj.com
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pubmed:publicationType |
Journal Article,
In Vitro
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