Characterization of high-affinity receptors for truncated glucagon-like peptide-1 in rat gastric glands.
The truncated form of glucagon-like peptide-1 (TGLP-1, or proglucagon 78-108), secreted by the mammalian intestine, has potent pharmacological activities, stimulating insulin release and inhibiting gastric acid secretion. We have characterized high-affinity receptors for this peptide in rat isolated fundic glands. Scatchard analysis of binding studies using mono-125I-TGLP-1(7-36) amide as tracer showed a single class of binding site of Kd (4.4 +/- (SE) .08) x 10(-10) M, with a tissue concentration of 1.0 +/- 0.1 fmol sites/microgram DNA. Whole GLP-1 was approximately 700 times less potent in displacing tracer, while human GLP-2 and pancreatic glucagon produced no significant displacement at concentrations up to 10(-6) M. The data support a physiological role for TGLP-1 in the regulation of gastric acid secretion.
Uttenthal
L O
LO
Department of Biochemistry and Molecular Biology, Faculty of Medicine, Universidad Complutense de Madrid, Ciudad Universitaria, Spain.
Blázquez
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E
D000818:Animals; D000242:Cyclic AMP / Q000096:biosynthesis; D005744:Gastric Acid / Q000378:metabolism; D005753:Gastric Mucosa / Q000032:analysis*; D005934:Glucagon / Q000378:metabolism* / Q000494:pharmacology; D052216:Glucagon-Like Peptide 1; D066298:In Vitro Techniques; D008297:Male; D010446:Peptide Fragments / Q000378:metabolism* / Q000494:pharmacology; D011498:Protein Precursors / Q000378:metabolism* / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D011956:Receptors, Cell Surface / Q000032:analysis*
D010446:Peptide Fragments; D011498:Protein Precursors; D011956:Receptors, Cell Surface; D052216:Glucagon-Like Peptide 1; D005934:Glucagon; D000242:Cyclic AMP