FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2011182974> ?p ?o ?g. }

• W2011182974 endingPage "1462" @default.
• W2011182974 startingPage "1451" @default.
• W2011182974 abstract "The mouse somatostatin (somatotropin release inhibiting factor, SRIF) sst5 receptor coding sequence was cloned from a mouse BALB/c genomic library. It shows 97% and 81% homology with the corresponding rat and human receptors, respectively. The msst5 receptor messenger RNA (mRNA) is present at low levels in the adult mouse brain, with significant expression in a few nuclei only, e.g. in the septum (lateral septal nuclei) or the amygdala (medial amygdaloid nucleus); very few signals were observed in the mesencephalon, metencephalon, and myelencephalon (except the dorsal motor nucleus of the vagus nerve). The msst5 receptor was stably expressed in the hamster fibroblast cell line CCL39-SRE-Luci, which harbours the luciferase reporter gene driven by the serum responsive element. [125I]LTT-SRIF-28 ([Leu8, D-Trp22, 125I-Tyr25]-SRIF-28), [125I]Tyr10-CST, [125I]CGP 23996, and [125I]Tyr3-octreotide labelled msst5 receptors with high affinity (pKd values: 11.0, 10.15, 9.75 and 9.43) and in a saturable manner, but defined different Bmax values: 697, 495, 540 and 144 fmoles/mg, respectively. [125I]LTT-SRIF-28-labelled sites displayed the following rank order: SRIF-28> rCST-14> somatuline > CGP-23996= SRIF-14= octreotide, whereas [125I]Tyr3-octreotide-labelled sites displayed a different profile: octreotide > SRIF-28> rCST-14= somatuline > SRIF-14> CGP-23996. The pharmacological profiles determined with [125I]LTT-SRIF-28, [125I]CGP 23996 and [125I]Tyr10-CST correlated highly significantly (r2 =0.88–0.99), whereas [125I]Tyr3-octreotide binding was rather divergent (r2 =0.77). Also, human and mouse sst5 receptor profiles are very different, e.g. r2 =0.385 for [125I]Tyr10-CST and r2 =0.323 for [125I]LTT-SRIF-28-labelled sites. Somatostatin induces expression of luciferase reporter gene in CCL39-SRE-Luci cells. The profile was consistent with a msst5 receptor-mediated effect although apparent potency in the luciferase assay was much reduced compared to radioligand binding data: Octreotide = SRIF-28> rCST-14= SRIF-14= CGP-23996. Octreotide, SRIF-28, BIM23052 and D Tyr Cyanamid 154806 behaved as full or nearly full agonists in comparison to SRIF-14, whereas the other compounds had relative efficacies of 40 to 70%. The present study shows that agonists radioligands define apparently different receptor populations in terms of number of sites and pharmacological profile in cells expressing a single recombinant receptor. These variations suggest that the conformation of the ligand receptor complex may vary depending on the agonist. Further, the msst5 receptor, although primarily coupled to Gi/Go proteins, is able to stimulate luciferase gene expression driven by the serum responsive element. Finally, it is suggested that putative sst2 selective agonists e.g. octreotide, RC160 or BIM23027 show similar or higher potency at msst5 receptors than SRIF-14." @default.
• W2011182974 created "2016-06-24" @default.
• W2011182974 creator A5007920388 @default.
• W2011182974 creator A5025503202 @default.
• W2011182974 creator A5025771885 @default.
• W2011182974 creator A5053148889 @default.
• W2011182974 creator A5056065387 @default.
• W2011182974 creator A5076877360 @default.
• W2011182974 creator A5085079447 @default.
• W2011182974 creator A5089197450 @default.
• W2011182974 date "2000-07-01" @default.
• W2011182974 modified "2023-10-10" @default.
• W2011182974 title "Cloning, expression and pharmacological characterisation of the mouse somatostatin sst5 receptor" @default.
• W2011182974 cites W1603788311 @default.
• W2011182974 cites W1963498145 @default.
• W2011182974 cites W1965615942 @default.
• W2011182974 cites W1985189889 @default.
• W2011182974 cites W1987776630 @default.
• W2011182974 cites W2006058334 @default.
• W2011182974 cites W2018491735 @default.
• W2011182974 cites W2032050038 @default.
• W2011182974 cites W2032515982 @default.
• W2011182974 cites W2066279507 @default.
• W2011182974 cites W2071127897 @default.
• W2011182974 cites W2073140573 @default.
• W2011182974 cites W2077054785 @default.
• W2011182974 cites W2082246436 @default.
• W2011182974 cites W2085402693 @default.
• W2011182974 cites W2118631824 @default.
• W2011182974 cites W2131690895 @default.
• W2011182974 cites W2406709103 @default.
• W2011182974 cites W4251915700 @default.
• W2011182974 cites W4293247451 @default.
• W2011182974 doi "https://doi.org/10.1016/s0028-3908(00)00063-0" @default.
• W2011182974 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/10818261" @default.
• W2011182974 hasPublicationYear "2000" @default.
• W2011182974 type Work @default.
• W2011182974 sameAs 2011182974 @default.
• W2011182974 citedByCount "36" @default.
• W2011182974 countsByYear W20111829742012 @default.
• W2011182974 countsByYear W20111829742015 @default.
• W2011182974 countsByYear W20111829742018 @default.
• W2011182974 countsByYear W20111829742019 @default.
• W2011182974 countsByYear W20111829742020 @default.
• W2011182974 crossrefType "journal-article" @default.
• W2011182974 hasAuthorship W2011182974A5007920388 @default.
• W2011182974 hasAuthorship W2011182974A5025503202 @default.
• W2011182974 hasAuthorship W2011182974A5025771885 @default.
• W2011182974 hasAuthorship W2011182974A5053148889 @default.
• W2011182974 hasAuthorship W2011182974A5056065387 @default.
• W2011182974 hasAuthorship W2011182974A5076877360 @default.
• W2011182974 hasAuthorship W2011182974A5085079447 @default.
• W2011182974 hasAuthorship W2011182974A5089197450 @default.
• W2011182974 hasConcept C118303440 @default.
• W2011182974 hasConcept C126322002 @default.
• W2011182974 hasConcept C134018914 @default.
• W2011182974 hasConcept C153911025 @default.
• W2011182974 hasConcept C170493617 @default.
• W2011182974 hasConcept C19519825 @default.
• W2011182974 hasConcept C2776297358 @default.
• W2011182974 hasConcept C2781025020 @default.
• W2011182974 hasConcept C71924100 @default.
• W2011182974 hasConcept C80115893 @default.
• W2011182974 hasConcept C86803240 @default.
• W2011182974 hasConceptScore W2011182974C118303440 @default.
• W2011182974 hasConceptScore W2011182974C126322002 @default.
• W2011182974 hasConceptScore W2011182974C134018914 @default.
• W2011182974 hasConceptScore W2011182974C153911025 @default.
• W2011182974 hasConceptScore W2011182974C170493617 @default.
• W2011182974 hasConceptScore W2011182974C19519825 @default.
• W2011182974 hasConceptScore W2011182974C2776297358 @default.
• W2011182974 hasConceptScore W2011182974C2781025020 @default.
• W2011182974 hasConceptScore W2011182974C71924100 @default.
• W2011182974 hasConceptScore W2011182974C80115893 @default.
• W2011182974 hasConceptScore W2011182974C86803240 @default.
• W2011182974 hasIssue "8" @default.
• W2011182974 hasLocation W20111829741 @default.
• W2011182974 hasLocation W20111829742 @default.
• W2011182974 hasOpenAccess W2011182974 @default.
• W2011182974 hasPrimaryLocation W20111829741 @default.
• W2011182974 hasRelatedWork W1741250325 @default.
• W2011182974 hasRelatedWork W1963723106 @default.
• W2011182974 hasRelatedWork W1994215581 @default.
• W2011182974 hasRelatedWork W2008562659 @default.
• W2011182974 hasRelatedWork W204194975 @default.
• W2011182974 hasRelatedWork W2047764997 @default.
• W2011182974 hasRelatedWork W2049160758 @default.
• W2011182974 hasRelatedWork W2140741951 @default.
• W2011182974 hasRelatedWork W2375763346 @default.
• W2011182974 hasRelatedWork W3216403534 @default.
• W2011182974 hasVolume "39" @default.
• W2011182974 isParatext "false" @default.
• W2011182974 isRetracted "false" @default.
• W2011182974 magId "2011182974" @default.
• W2011182974 workType "article" @default.