Abstract
MA1050 is distributed in tissues as a typical organic base and excreted primarily in urine. Repeated treatment of rats does not result in marked alteration of tissue distribution, although excretion is prolonged, and the relative importance of the urinary and fecal routes is altered. The reduced (cyclohexanol) derivative of MA1050 and a metabolite presumed to be its O -glucuronide are found in urine, along with an additional unidentified metabolite. The major urinary metabolites may be the p -and/or o -phenolic derivatives of the Mannich base. Mannich hydrolysis was not shown to occur to a significant extent, and the suggestion that products of Mannich hydrolysis might be responsible for the ocular toxicity elicited by MA1050 was not supported.
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