Über den Metabolismus eines cytostatisch wirksamen Methylhydrazin-Derivates (Natulan)

Determination of terephthalic acid isopropylamide in urine with a liquid chromatography/mass spectrometry (LC/MS) method

“…Terephthalic acid isopropylamide is the major urinary metabolite of procarbazine (1,2). The urinary excretion of procarbazine in human beings, dogs, and rats is extensive, with 67-70% of the administrated dose excreted in the urine within 24 hr measured as a radio-labeled fraction (3).…”

Metabolic Fate of Hydrazines and Hydrazides

“…The hypothesis of Dost and Reed has been greatly strengthened by the demonstration of N-isopropylterephthalmic acid (VII) (18)(19)(20) as a metabolite of MIH. N-Isopropylterephthalamic acid is formed quite rapidly from MIH and can be demonstrated in the urine 10 min.…”

“…Within 8 hr. after administration, 7-10% of the dose was expired as 14CH4 and 11-22% was expired as 14C02 (18). The H,NNHZ -CH,CONHNHCCCH, (Eq.…”

Antimitotic Activity of the Methylhydrazine Derivative Natulan® in the Ehrlich Ascites Carcinoma; Dose-effect Relationship

“…Consequently it seems obvious that the compound is rapidly metabolized as has been shown in several animals [14,19]. The delayed antimitotic action which could be exerted by the formic alde hyde as a metabolite according to W e it z e l [19,20] is not applicable to Ehrlich ascites carcinoma.…”

“…In fact its biological action takes place through inhibition not only of D NA and RNA synthesis but also of protein synthesis by inter ference with the incorporation of the amino acids glycine, leucine and valine into tumor cell proteins [7,14,18]. Furthermore the compound seems to inhibit certain enzymes participating in glucose metabolism [10,13].…”