Source:http://linkedlifedata.com/resource/pubmed/id/12065886
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
6
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| pubmed:dateCreated |
2002-6-14
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| pubmed:abstractText |
Somatostatin (SRIH) regulates pituitary adrenocorticotropin (ACTH) secretion by interacting with a family of homologous G protein-coupled membrane receptors. The SRIH receptor subtypes (sst(1)-sst(5)) that control ACTH release remain unknown. Using novel, subtype-selective SRIH analogs, we have identified the SRIH receptor subtypes involved in regulating ACTH release from AtT-20 cells, a model for cell line pituitary corticotropes. Radioligand-binding studies with (125)I-SRIH-14 and (125)I-SRIH-28 showed that SRIH-14 and SRIH-28 recognized specific, high-affinity and saturable membrane-binding sites. Nonpeptidyl agonists with selectivity for the sst(2) (L-779,976; compound 2) or sst(1)/sst(5)) (L-817,818; compound 5) receptor subtypes potently displaced (125)I-SRIH-28 from AtT-20 cell membranes, while agonists selective for the sst(1) (L-779,591; compound 1), sst(3) (L-796,778; compound 3) or sst(4) (L-803,087; compound 4) subtypes were inactive. Tyr(11)-SRIH-14, compound 2 (sst(2)) or compound 5 (sst(5)) inhibited forskolin and corticotropin-releasing hormone (CRH)-induced increases in intracellular cAMP. Furthermore, the sst(2) and sst(5) agonists potently inhibited CRH-induced ACTH release from AtT-20 cells. These results provide the first evidence that sst(2) and sst(5) receptor subtypes, but not sst(1), sst(3) or sst(4), inhibit cAMP accumulation and regulate ACTH secretion in the AtT-20 cell model of the rodent corticotrope.
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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/Adrenocorticotropic Hormone,
http://linkedlifedata.com/resource/pubmed/chemical/Corticotropin-Releasing Hormone,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclic AMP,
http://linkedlifedata.com/resource/pubmed/chemical/Fungal Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/GTPase-Activating Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Iodine Radioisotopes,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Somatostatin,
http://linkedlifedata.com/resource/pubmed/chemical/SST2 protein, S cerevisiae,
http://linkedlifedata.com/resource/pubmed/chemical/Saccharomyces cerevisiae Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Somatostatin,
http://linkedlifedata.com/resource/pubmed/chemical/Somatostatin-28,
http://linkedlifedata.com/resource/pubmed/chemical/somatostatin receptor 5
|
| pubmed:status |
MEDLINE
|
| pubmed:month |
Jun
|
| pubmed:issn |
0028-3835
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| pubmed:author | |
| pubmed:copyrightInfo |
Copyright 2002 S. Karger AG, Basel
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| pubmed:issnType |
Print
|
| pubmed:volume |
75
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| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
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| pubmed:pagination |
339-46
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| pubmed:dateRevised |
2006-11-15
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| pubmed:meshHeading |
pubmed-meshheading:12065886-Adrenocorticotropic Hormone,
pubmed-meshheading:12065886-Binding, Competitive,
pubmed-meshheading:12065886-Cell Line,
pubmed-meshheading:12065886-Corticotropin-Releasing Hormone,
pubmed-meshheading:12065886-Cyclic AMP,
pubmed-meshheading:12065886-Fungal Proteins,
pubmed-meshheading:12065886-GTPase-Activating Proteins,
pubmed-meshheading:12065886-Iodine Radioisotopes,
pubmed-meshheading:12065886-Pituitary Gland,
pubmed-meshheading:12065886-Radioligand Assay,
pubmed-meshheading:12065886-Receptors, Somatostatin,
pubmed-meshheading:12065886-Saccharomyces cerevisiae Proteins,
pubmed-meshheading:12065886-Somatostatin,
pubmed-meshheading:12065886-Somatostatin-28
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| pubmed:year |
2002
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| pubmed:articleTitle |
Somatostatin receptor subtypes 2 and 5 inhibit corticotropin-releasing hormone-stimulated adrenocorticotropin secretion from AtT-20 cells.
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| pubmed:affiliation |
Merck Research Laboratories, Rahway, NJ, USA.
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| pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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