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rdf:type |
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lifeskim:mentions |
umls-concept:C0002482,
umls-concept:C0007634,
umls-concept:C0008109,
umls-concept:C0021670,
umls-concept:C0030956,
umls-concept:C0060993,
umls-concept:C0231491,
umls-concept:C0243192,
umls-concept:C0441472,
umls-concept:C0972293,
umls-concept:C1167622
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pubmed:issue |
3
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pubmed:dateCreated |
1996-3-14
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pubmed:abstractText |
The chimeric peptide M35 [galanin(1-13)-bradykinin(2-9) amide] is a high-affinity galanin receptor ligand acting as a galanin receptor antagonist in the rat spinal cord, rat hippocampus and isolated mouse pancreatic islets. We have radiolabelled M35 and performed equilibrium binding studies with [125I]M35 on the rat pancreatic beta-cell line Rin m 5F, whereby we show the existence of high-affinity binding site (KD = 0.9 +/- 0.1 nM) with a Bmax of 72 +/- 3 fmol/mg protein. Galanin displaces [125I]M35 with the same affinity (KD = 1 nM) as it displaces [125I]galanin. Displacement of [125I]galanin by M35 from Rin m 5F cell membranes shows the presence of two binding sites for M35 with KD-values of 0.3 +/- 0.1 nM and 0.52 +/- 0.03 microM, respectively. The GTP- and pertussis toxin-sensitivity of M35 binding to Rin m 5F membranes shows that binding of [125I]M35 is almost completely abolished by the presence of GTP or after pertussis toxin treatment of the cells, indicating an agonist-like binding of M35 to the galanin receptors. M35 has a dual effect on the galanin mediated inhibition of forskolin stimulated cyclic AMP production in Rin m 5F cells: at low concentrations M35 antagonises the effect of galanin, whereas at concentrations above 10 nM M35 acts as a galanin receptor agonist. These agonist-like effects of galanin and M35 are not additive, thus the mixed agonist/antagonist properties arise from the chimeric nature of M35[galanin(1-13)-bradykinin(2-9)amide] acting solely at galanin receptors.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Bradykinin,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclic AMP,
http://linkedlifedata.com/resource/pubmed/chemical/Forskolin,
http://linkedlifedata.com/resource/pubmed/chemical/Galanin,
http://linkedlifedata.com/resource/pubmed/chemical/Guanosine Triphosphate,
http://linkedlifedata.com/resource/pubmed/chemical/Ligands,
http://linkedlifedata.com/resource/pubmed/chemical/Peptide Fragments,
http://linkedlifedata.com/resource/pubmed/chemical/Pertussis Toxin,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Galanin,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Gastrointestinal Hormone,
http://linkedlifedata.com/resource/pubmed/chemical/Recombinant Fusion Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Virulence Factors, Bordetella,
http://linkedlifedata.com/resource/pubmed/chemical/galanin-(1-13)-bradykinin-(2-9)-amid...
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
0167-0115
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
10
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pubmed:volume |
59
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
341-8
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:8577939-Animals,
pubmed-meshheading:8577939-Binding, Competitive,
pubmed-meshheading:8577939-Binding Sites,
pubmed-meshheading:8577939-Bradykinin,
pubmed-meshheading:8577939-Cell Membrane,
pubmed-meshheading:8577939-Cyclic AMP,
pubmed-meshheading:8577939-Forskolin,
pubmed-meshheading:8577939-Galanin,
pubmed-meshheading:8577939-Guanosine Triphosphate,
pubmed-meshheading:8577939-Insulinoma,
pubmed-meshheading:8577939-Ligands,
pubmed-meshheading:8577939-Peptide Fragments,
pubmed-meshheading:8577939-Pertussis Toxin,
pubmed-meshheading:8577939-Protein Binding,
pubmed-meshheading:8577939-Rats,
pubmed-meshheading:8577939-Receptors, Galanin,
pubmed-meshheading:8577939-Receptors, Gastrointestinal Hormone,
pubmed-meshheading:8577939-Recombinant Fusion Proteins,
pubmed-meshheading:8577939-Tumor Cells, Cultured,
pubmed-meshheading:8577939-Virulence Factors, Bordetella
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pubmed:year |
1995
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pubmed:articleTitle |
Binding and agonist/antagonist actions of M35, galanin(1-13)-bradykinin(2-9)amide chimeric peptide, in Rin m 5F insulinoma cells.
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pubmed:affiliation |
Department of Neurochemistry and Neurotoxicology, Arrhenius Laboratories, Stockholm University, Sweden.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Research Support, Non-U.S. Gov't
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