Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
2001-5-2
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.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Apr
pubmed:issn
0213-3911
pubmed:author
pubmed:issnType
Print
pubmed:volume
16
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
535-40
pubmed:dateRevised
2006-11-15
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
pubmed:year
2001
pubmed:articleTitle
Endothelin-1[1-31] acts as a selective ETA-receptor agonist in the rat adrenal cortex.
pubmed:affiliation
Department of Human Anatomy and Physiology, Padua, Italy.
pubmed:publicationType
Journal Article, In Vitro