[HTML][HTML] Characterization of a novel, non-peptidyl antagonist of the human glucagon receptor
MA Cascieri, GE Koch, E Ber, SJ Sadowski… - Journal of Biological …, 1999 - ASBMB
We have identified a series of potent, orally bioavailable, non-peptidyl, triarylimidazole and
triarylpyrrole glucagon receptor antagonists. 2-(4-Pyridyl)-5-(4-chlorophenyl)-3-(5-bromo-2-
propyloxyphenyl) pyrrole (L-168,049), a prototypical member of this series, inhibits binding
of labeled glucagon to the human glucagon receptor with an IC 50= 3.7±3.4 nm (n= 7) but
does not inhibit binding of labeled glucagon-like peptide to the highly homologous human
glucagon-like peptide receptor at concentrations up to 10 μm. The binding affinity of L …
triarylpyrrole glucagon receptor antagonists. 2-(4-Pyridyl)-5-(4-chlorophenyl)-3-(5-bromo-2-
propyloxyphenyl) pyrrole (L-168,049), a prototypical member of this series, inhibits binding
of labeled glucagon to the human glucagon receptor with an IC 50= 3.7±3.4 nm (n= 7) but
does not inhibit binding of labeled glucagon-like peptide to the highly homologous human
glucagon-like peptide receptor at concentrations up to 10 μm. The binding affinity of L …