TY - JOUR T1 - 3-(Hydroxymethyl)-8-methoxychromone and unconjugated metabolites in rat plasma. Identification of the biologically active species. JF - Drug Metabolism and Disposition JO - Drug Metab Dispos SP - 368 LP - 371 VL - 4 IS - 4 AU - F J De Carlo AU - D J Herzig AU - E J Kusner AU - P R Schumann AU - M D Melgar AU - S George AU - M C Crew Y1 - 1976/07/01 UR - http://dmd.aspetjournals.org/content/4/4/368.abstract N2 - After administering 14C-labeled 3-(hydroxymethyl)-8-methoxychromone to rats by gavage, plasma was found to contain unchanged compound and three unconjugated metabolites. These metabolites were identified as 3-carboxy-8-methoxychromone, 8-methoxychromone, and 2-hydroxy-3-methoxyactophenone. The plasma levels of all four labeled compounds were determined from 30 min to 48 hr after drug administration. Only the levels of 3-(hydroxymethyl)-8-methoxychromone and 3-carboxy-8-methoxychromone correlated with the expression of antiallergy activity in the rat, and only these compounds were found to be active in vivo. However, a test system for the inhibition of anaphylactic histamine release in vitro showed activity only for 3-carboxy-8-methoxychromone. ER -