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Abstract
1. The metabolism of imiloxan hydrochloride [(±)-2-(1-ethyl-2-imidazoyl)methyl-1,4-benzodioxane hydrochloride], an α2-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).