PT  - JOURNAL ARTICLE
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
TI  - 3-(Hydroxymethyl)-8-methoxychromone and unconjugated metabolites in rat plasma. Identification of the biologically active species.
DP  - 1976 Jul 01
TA  - Drug Metabolism and Disposition
PG  - 368--371
VI  - 4
IP  - 4
4099  - http://dmd.aspetjournals.org/content/4/4/368.short
4100  - http://dmd.aspetjournals.org/content/4/4/368.full
SO  - Drug Metab Dispos1976 Jul 01; 4
AB  - 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.