AI Article Synopsis
- The study focused on the metabolism of imiloxan hydrochloride, an alpha 2-adrenoceptor antagonist, in four male volunteers after a single oral dose of 500 mg.
- Most of the compound-related radioactivity was quickly eliminated in urine within 24 hours, indicating rapid metabolism.
- Key urinary metabolites included various oxidized forms and conjugates of imiloxan, with the major ones constituting 37-41% of the dose, highlighting the compound's metabolic pathways.
Article Abstract
1. The metabolism of imiloxan hydrochloride [(+-)-2-(1-ethyl-2-imidazoyl)methyl-1,4-benzodioxane hydrochloride], an alpha 2-adrenoceptor antagonist, was studied in four male volunteers given a 500 mg oral dose containing 0.48 MBq of the 14C-labelled material. Compound-related radioactivity was rapidly excreted chiefly in the urine within 24 h of dosing. 2. Metabolites derived by initial oxidation on either or both the benzodioxane and imidazoyl moieties followed by glucuronic acid and sulphate conjugation, and an N-glucuronide of imiloxan were tentatively identified in urine. 3. The major urinary metabolites, comprising some 37-41% of the dose, appeared to be +-2-(1-ethyl-2-imidazoyl)methyl-1,4-benzodioxane-6/7-sulphonic acid (19% of dose), [+-2-(1-ethyl-2-imidazoyl)methyl-1,4-benzodioxane- 6/7-ylium D-glucopyranoside]uronate (10-14% of dose), and a glucuronide conjugate of +-2-(1-ethyl-2-imidazoyl-4/5-hydroxy)methyl-1,4-benzodioxane (8% of dose).
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| http://dx.doi.org/10.3109/00498259209046622 | DOI Listing |
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