Source:http://linkedlifedata.com/resource/pubmed/id/11284447
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
3
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| pubmed:dateCreated |
2001-4-3
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| pubmed:abstractText |
Although thoracic and abdominal rat aorta are often used as a classical pharmacological preparation for the assessment of vascular drug effects, little is known on regional differences among these two parts of the aorta with regard to their reaction to Gq/11-coupled receptor activation. Thus, we determined, in rings from thoracic and abdominal aorta from 12-week-old male Wistar rats, the effects of noradrenaline (NA; 10(-8)-10(-4) M), endothelin-1 (ET-1; 10(-10)-10(-6) M) and the thromboxane A2 mimetic U 46619 (10(-8)-10(-5) M) on inositolphoshate (IP) formation (assessed as accumulation of total [3H]IPs in [3H]myoinositol prelabelled rings). NA, ET-1 and U 46619 concentration-dependently increased IP formation; maximum increases were, however, significantly more pronounced in thoracic than in abdominal aorta. Similarly, NA, ET-1 and U 46619 evoked significantly larger maximum contractions in thoracic than in abdominal aorta. NA-induced [3H]IP formation could be inhibited with BMY 7378 (10(-9)-10(-4) M) and with 5-methyl-urapidil (5-MU; 10(-9)-10(-5) M) both exhibiting biphasic concentration-inhibition curves. The pKi-values for BMY 7378 at the high affinity site were in thoracic aorta 8.93+/-0.28 (n=5), and in abdominal aorta 8.76+/-0.35 (n=4) and at the low affinity site 6.45+/-0.2 (thoracic aorta) and 6.55+/-0.27 (abdominal aorta). pKi-Values for 5-MU in thoracic aorta at the high affinity site were 8.25+/-0.34 (n=4), and at the low affinity site 6.61+/-0.39 . In abdominal aorta reliable pKi-values could not be calculated for 5-MU due to a low signal-to-noise ratio. On the other hand, in both preparations the ETA-receptor antagonist BQ-123 (10(-9)-10(-5) M) and the TP-receptor antagonist SQ 29548 (10(-9)-10(-5) M) inhibited ET-1- and U 46619-induced IP formation, respectively, with monophasic concentration-inhibition curves: pKi-values for BQ-123 were: 8.16+/-0.24 (thoracic aorta) and 8.10+/-0.35 (abdominal aorta) and for SQ 29548: 8.2+/-0.3 (thoracic aorta) and 8.5+/-0.3 (abdominal aorta). The amount of immunodetectable Gq/11-protein was similar in both tissues. We conclude that responses to NA, ET-1 and U 46619 (IP formation and contractile force) are larger in thoracic than in abdominal aorta. ET-1 effects on IP formation are mediated by ETA-receptors and U 46619 effects by TP-receptors. NA effects are mediated by alpha1D- and alpha1A-adrenoceptors; alpha1B-adrenoceptors seem to play a minor role.
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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/15-Hydroxy-11 alpha,9...,
http://linkedlifedata.com/resource/pubmed/chemical/5-methylurapidil,
http://linkedlifedata.com/resource/pubmed/chemical/Adrenergic alpha-Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/Adrenergic alpha-Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/BMY 7378,
http://linkedlifedata.com/resource/pubmed/chemical/Clonidine,
http://linkedlifedata.com/resource/pubmed/chemical/Endothelin-1,
http://linkedlifedata.com/resource/pubmed/chemical/GTP-Binding Protein alpha...,
http://linkedlifedata.com/resource/pubmed/chemical/Heterotrimeric GTP-Binding Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Inositol Phosphates,
http://linkedlifedata.com/resource/pubmed/chemical/Norepinephrine,
http://linkedlifedata.com/resource/pubmed/chemical/Peptides, Cyclic,
http://linkedlifedata.com/resource/pubmed/chemical/Piperazines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Endothelin A,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, alpha,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Endothelin,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Thromboxane,
http://linkedlifedata.com/resource/pubmed/chemical/Vasoconstrictor Agents,
http://linkedlifedata.com/resource/pubmed/chemical/chlorethylclonidine,
http://linkedlifedata.com/resource/pubmed/chemical/cyclo(Trp-Asp-Pro-Val-Leu)
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| pubmed:status |
MEDLINE
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| pubmed:month |
Mar
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| pubmed:issn |
0028-1298
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| pubmed:author | |
| pubmed:issnType |
Print
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| pubmed:volume |
363
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| pubmed:owner |
NLM
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| pubmed:authorsComplete |
Y
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| pubmed:pagination |
322-9
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| pubmed:dateRevised |
2009-11-19
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| pubmed:meshHeading |
pubmed-meshheading:11284447-15-Hydroxy-11 alpha,9...,
pubmed-meshheading:11284447-Adrenergic alpha-Agonists,
pubmed-meshheading:11284447-Adrenergic alpha-Antagonists,
pubmed-meshheading:11284447-Animals,
pubmed-meshheading:11284447-Aorta, Abdominal,
pubmed-meshheading:11284447-Aorta, Thoracic,
pubmed-meshheading:11284447-Clonidine,
pubmed-meshheading:11284447-Endothelin-1,
pubmed-meshheading:11284447-GTP-Binding Protein alpha Subunits, Gq-G11,
pubmed-meshheading:11284447-Heterotrimeric GTP-Binding Proteins,
pubmed-meshheading:11284447-Inositol Phosphates,
pubmed-meshheading:11284447-Male,
pubmed-meshheading:11284447-Muscle Contraction,
pubmed-meshheading:11284447-Norepinephrine,
pubmed-meshheading:11284447-Peptides, Cyclic,
pubmed-meshheading:11284447-Piperazines,
pubmed-meshheading:11284447-Rats,
pubmed-meshheading:11284447-Rats, Wistar,
pubmed-meshheading:11284447-Receptor, Endothelin A,
pubmed-meshheading:11284447-Receptors, Adrenergic, alpha,
pubmed-meshheading:11284447-Receptors, Endothelin,
pubmed-meshheading:11284447-Receptors, Thromboxane,
pubmed-meshheading:11284447-Vasoconstrictor Agents
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| pubmed:year |
2001
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| pubmed:articleTitle |
Inositolphosphate formation in thoracic and abdominal rat aorta following Gq/11-coupled receptor stimulation.
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| pubmed:affiliation |
Institute of Pharmacology, University of Halle-Wittenberg, Halle/Saale, Germany. stefan.dhein@medizin.uni-halle.de
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| pubmed:publicationType |
Journal Article,
Comparative Study,
In Vitro,
Research Support, Non-U.S. Gov't
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