Investigations into the metabolic fate and distribution of Hepzidine (cas 1096-72-6) maleate in the rat and the mouse

Add time:08/12/2019    Source:sciencedirect.com

Metabolic studies with Hepzidine (cas 1096-72-6) maleate, labelled in two positions with 3H and 14C, respectively, showed that in rats, over 50 per cent of an orally administered dose of hepzidine maleate (10 mgkg) is hydrolysed before absorption. The nonhydrolysed part of the dose is absorbed to a large extent. An important biotransformation of hepzidine is N-demethylation; it involves about 20 per cent of a 10-mgkg oral dose and over 37 per cent of an equal dose, given i.p. On the other hand, N-demethylation of the hydrolytic product 1-methyl-4-piperidinol was very slight. Excretion of 14C radioactivity in the expired air shows good first-order kinetics, from which a half-life of about 4.2 hr could be evaluated for hepzidine maleate in the rat. Next to urinary excretion, biliary excretion plays an important role in the elimination of hepzidine maleate and metabolites. In the urine the hydrolytic products of hepzidine, especially 1-methyl-4-piperidinol and its metabolites (probably conjugates) are predominant. There is evidence that in bile the hydrolytic product 10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-ol and its metabolites (probably conjugates) are predominant, but in contrast to urine a substantial amount of the hepzidine is excreted in bile as such and/or in some form which still possesses the intact hepzidine structure. After i.p. administration of hepzidine maleate-14C to female mice (50 mgkg) autoradiographic distribution studies show the radioactivity to attain considerable levels in most organs, while blood levels stay relatively low. Highest accumulations of radioactivity are found in the liver, lungs, hypophysis, Harder's gland, submaxillary gland, mucous glands in tongue, palatum and pharynx, bone marrow, lymphoid tissue, urinary bladder wall, urine, bile, intestinal contents, and specified zones in the kidneys and adrenals. To a lesser degree there is also a pronounced penetration of radioactivity into the CNS, where hippocampus, cerebral cortex and thalamus show a higher degree of radioactivity than other brain areas. In most organs maximum levels are observed at 1 hr after administration. No specific long-lasting accumulations of radioactivity have been observed, except in the urinary bladder wall, which still shows a high level of radioactivity at 16 hr after administration.

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