Article
Characterization of a novel, non-peptidyl antagonist of the human glucagon receptor.
The Journal of biological chemistry - 26 Mar 1999
Cascieri M A, Koch G E, Ber E, Sadowski S J, Louizides D, de Laszlo S E, Hacker C, Hagmann W K, MacCoss M, Chicchi G G, Vicario P P
Abstract excerpt
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)p yrr ole (L-168,049), a prototypical member of this series, inhibits binding of labeled glucagon to the human glucagon receptor with an IC50 = 3. 7 +/- 3.4 nM (n = 7) but does not inhibit binding of labeled...
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