RT Journal Article
SR Electronic
T1 The metabolism of avermectins B1a, H2B1a, and H2B1b by liver microsomes.
JF Drug Metabolism and Disposition
JO Drug Metab Dispos
FD American Society for Pharmacology and Experimental Therapeutics
SP 268
OP 274
VO 10
IS 3
A1 G T Miwa
A1 J S Walsh
A1 W J VandenHeuvel
A1 B Arison
A1 E Sestokas
A1 R Buhs
A1 A Rosegay
A1 S Avermitilis
A1 A Y Lu
A1 M A Walsh
A1 R W Walker
A1 R Taub
A1 T A Jacob
YR 1982
UL http://dmd.aspetjournals.org/content/10/3/268.abstract
AB The avermectins area a new class of structurally related antiparasitic agents isolated from Streptomyces avermitilis. The major polar metabolites isolated from in vitro incubations of [3H]avermectins B1a, H2B1a, and H2B1b with either rat or steer liver microsomes have been isolated and identified as the C24-methyl alcohols of the parent compounds. A smaller quantity of a more polar metabolite has also been identified as the monosaccharide of the C24-methyl alcohols of avermectin H2H1b from rat liver microsomal incubation and avermectin H2B1a from steer liver microsomal incubation. The mass spectra and 300-MHz 1H-NMR spectra permitted assignment of structures to these metabolites. Together these two metabolites represent 50-80% of the total radioactivity more polar than the parent compounds. The metabolite profiles on reverse-phase HPLC demonstrate that the rat and steer are qualitatively similar in the production of these two polar metabolites.