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Exendin-3 (9-39) amide
Biological Activity:
Potent
and selective GLP-1 receptor antagonist (Kd = 1.7 nM at cloned human
GLP-1 receptor). Inhibits cAMP production and insulin release induced by GLP-1
(7-36), exendin-3 (IC50 = 20 nM) and exendin-4. Blocks the
inhibitory effect of GLP-1 on food intake in rats.
Raufman
et al (1991) Exendin-3, a novel peptide
from the Heloderma horridum venom, interacts with vasoactive intestinal
peptide receptors and a newly described receptor on dispersed acini from guinea
pig pancreas. J.Biol.Chem. 266 2897. Gokeet al
(1993) Exendin-4 is a high potency agonist and truncated exendin-(9-39)-amide
an antagonist at the glucagon-like peptide 1-(7-36)-amide receptor of
insulin-secreting β-cells. J.Biol.Chem. 268 19650. Thorenset al
(1993) Cloning and functional expression of the human islet GLP-1 receptor.
Demonstration that exendin-4 is an agonist and exendin-(9-39) an antagonist of
the receptor. Diabetes 42 1678. Turtonet al (1996)
A role for glucagon-like peptide-1 in the central regulation of feeding. Nature
379 69.
