BAY U6751 is a glycogen phosphorylase inhibitor. Formed from the prodrug, BAYR3401. BAY U6751 exists as the enantiomeric mixture. BAY W1807 is the active metabolite.
BAY W1807, the active metabolite of BAY R3401, inhibits muscle glycogen phosphorylase a and b. In gel-filtered liver extracts, racemic BAY U6751 (containing active BAY W1807) was tested for inhibition of phosphorylase in the glycogenolytic (in which only phosphorylase a is active). In liver extracts, BAY U6751 (0.9-36 μmol/L) inhibited glycogen synthesis by phosphorylase b (notwithstanding the inclusion of AMP), but not by phosphorylase a. Inhibition of phosphorylase-a-catalyzed glycogenolysis was partially relieved by AMP (500 μmol/L). BAY U6751 facilitated phosphorylase-a dephosphorylation. Isolated hepatocytes and perfused livers were tested for BAY R3401-induced changes in phosphorylase-a:b ratios and glycogenolytic output.
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