Metabolism of 1-(3,4-dichlorobenzyl)-5- octylbiguanide in the dog

Abstract

1. The biotransformation of 1-(3,4-dichlorobenzyl)-5-octylbiguanide (OPB-2045), a new potent biguanide antiseptic, was investigated in male beagle dogs. Urinary and faecal excretion of unchanged compound and metabolites were studied following a single subcutaneous injection of ¹⁴C-labeled compound at a dose of 1 mg/kg. 2. Four urinary metabolites were structually identified using synthetic standards and orspectraldataas3,4-dichlorobenzoicacid,6-[5-(3,4-dichlorobenzyl)-1-biguanidino hexanoic acid (DM-210), 4-[5-(3,4-dichlorobenzyl)-1-biguanidino] butanoic acid (DM212) and 5-[5-(3,4-dichlorobenzyl)-1-biguanidino] pentanoic acid (DM-213). 3. The predominant radioactive substances in the excreta were DM-213 and DM-210 at 26 1% and 25 5%, respectively, of the dose. No unchanged compound was detected in the urine, and in the faeces it was only 2% of the dose.