title: Receptors for glucagon-like peptide-1(7-36) amide on rat insulinoma-derived cells.
abstract: Specific binding of 125I-labelled glucagon-like peptide-1(7-36)amide (GLP-1(7-36)amide) to rat insulinoma-derived RINm5F cells was dependent upon time and temperature and was proportional to cell concentration. Binding of radioactivity was inhibited in a concentration-dependent manner by GLP-1(7-36) amide consistent with the presence of a single class of binding site with a dissociation constant (Kd) of 204 +/- 8 pmol/l (mean +/- S.E.M.). Binding of the peptide resulted in a dose-dependent increase in cyclic AMP concentrations (half maximal response at 250 +/- 20 pmol/l). GLP-1(1-36)amide was approximately 200 times less potent than GLP-1(7-36)amide in inhibiting the binding of 125I-labelled GLP-1(7-36)amide to the cells (Kd of 45 +/- 6 nmol/l). Binding sites for GLP-1 (7-36)amide were not present on dispersed enterocytes from porcine small intestine.
authors.affiliation: Clinical Research Group for Gastrointestinal Endocrinology, University of Göttingen, Federal Republic of Germany.
authors.forename: R
authors.initials: R
authors.lastname: Göke
authors.forename: J M
authors.initials: JM
authors.lastname: Conlon
mesh_terms: D007516:Adenoma, Islet Cell / Q000032:analysis*; D000818:Animals; D001667:Binding, Competitive; D002460:Cell Line; D000242:Cyclic AMP / Q000096:biosynthesis; D005934:Glucagon; D052216:Glucagon-Like Peptide 1; D000067757:Glucagon-Like Peptide-1 Receptor; D004763:Glucagon-Like Peptides; D007340:Insulinoma / Q000032:analysis* / Q000378:metabolism; D007413:Intestinal Mucosa / Q000378:metabolism; D007583:Jejunum / Q000378:metabolism; D010190:Pancreatic Neoplasms / Q000032:analysis* / Q000378:metabolism; D010446:Peptide Fragments; D010455:Peptides / Q000378:metabolism*; D051381:Rats; D011956:Receptors, Cell Surface / Q000032:analysis; D018027:Receptors, Glucagon
chemical_list: C000593835:Glp1r protein, rat; D000067757:Glucagon-Like Peptide-1 Receptor; D010446:Peptide Fragments; D010455:Peptides; D011956:Receptors, Cell Surface; D018027:Receptors, Glucagon; C055453:glucagon-like peptide 1 (7-36)amide; D004763:Glucagon-Like Peptides; D052216:Glucagon-Like Peptide 1; D005934:Glucagon; C055454:glucagon-like peptide 1 (1-36)amide; D000242:Cyclic AMP