Source:http://linkedlifedata.com/resource/pubmed/id/11332709
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
2001-5-2
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pubmed:abstractText |
Endothelin-1 (ET-1) is a 21-amino acid residue (ET-1[1-21]) hypertensive peptide, which together with its receptor subtypes A and B (ETA and ETB) is expressed in the rat adrenal cortex, where it stimulates steroid-hormone (aldosterone and corticosterone) secretion through the ETB receptor and the growth (proliferative activity) of the zona glomerulosa (ZG) through the ETA receptor. ET-1[1-21] is generated from bigET-1 by the endothelin-converting enzyme (ECE-1). However, recent evidence indicates the existence of an alternative chymase-mediated biosynthetic pathway leading to the production of an ET-1[1-31] peptide, which was found to reproduce the ETA receptor-mediated vascular effects of ET-1[1-21]. We found that ET-1[1-21], but not ET-1[1-31], concentration-dependently raised steroid secretion from dispersed rat adrenocortical cells, its effect being blocked by the ETB-receptor selective antagonist BQ-788. Both ET-1s concentration-dependently increased the number of "S-phase" cells (as detected by the 5-bromo-2'-deoxyuridine immunocytochemical method) in capsule-ZG strips within a 240 min incubation. The ZG proliferogenic action of both ET-1s was blocked by the ETA-receptor antagonist BQ-123, and ET-1[1-31] was found to be significantly more potent than ET-1[1-21]. Autoradiography showed that in the rat adrenal ET-1[1-21] displaced the binding of selective ligands to both ETA ([125I]PD-151242) and ETB receptors ([125I]BQ-3020), while ET-1[1-31] eliminates only the binding to ETA receptors. Collectively, our findings provide strong evidence that ET-1[1-31] acts in the rat adrenal glands as a selective ETA-receptor agonist, mainly involved in the stimulation of ZG proliferative activity.
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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/Adrenal Cortex Hormones,
http://linkedlifedata.com/resource/pubmed/chemical/Bromodeoxyuridine,
http://linkedlifedata.com/resource/pubmed/chemical/Endothelin-1,
http://linkedlifedata.com/resource/pubmed/chemical/Enzyme Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Oligopeptides,
http://linkedlifedata.com/resource/pubmed/chemical/Peptide Fragments,
http://linkedlifedata.com/resource/pubmed/chemical/Peptides,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Endothelin
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
0213-3911
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
16
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
535-40
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:11332709-Adrenal Cortex,
pubmed-meshheading:11332709-Adrenal Cortex Hormones,
pubmed-meshheading:11332709-Adrenal Glands,
pubmed-meshheading:11332709-Animals,
pubmed-meshheading:11332709-Autoradiography,
pubmed-meshheading:11332709-Bromodeoxyuridine,
pubmed-meshheading:11332709-Cell Division,
pubmed-meshheading:11332709-Dose-Response Relationship, Drug,
pubmed-meshheading:11332709-Endothelin-1,
pubmed-meshheading:11332709-Enzyme Inhibitors,
pubmed-meshheading:11332709-Immunohistochemistry,
pubmed-meshheading:11332709-Male,
pubmed-meshheading:11332709-Oligopeptides,
pubmed-meshheading:11332709-Peptide Fragments,
pubmed-meshheading:11332709-Peptides,
pubmed-meshheading:11332709-Radioligand Assay,
pubmed-meshheading:11332709-Rats,
pubmed-meshheading:11332709-Rats, Sprague-Dawley,
pubmed-meshheading:11332709-Receptors, Endothelin,
pubmed-meshheading:11332709-S Phase,
pubmed-meshheading:11332709-Zona Glomerulosa
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pubmed:year |
2001
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pubmed:articleTitle |
Endothelin-1[1-31] acts as a selective ETA-receptor agonist in the rat adrenal cortex.
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pubmed:affiliation |
Department of Human Anatomy and Physiology, Padua, Italy.
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pubmed:publicationType |
Journal Article,
In Vitro
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