EurekaMag.com logo
+ Site Statistics
References:
53,869,633
Abstracts:
29,686,251
+ Search Articles
+ Subscribe to Site Feeds
EurekaMag Most Shared ContentMost Shared
EurekaMag PDF Full Text ContentPDF Full Text
+ PDF Full Text
Request PDF Full TextRequest PDF Full Text
+ Follow Us
Follow on FacebookFollow on Facebook
Follow on TwitterFollow on Twitter
Follow on LinkedInFollow on LinkedIn

+ Translate

Metabolic activation of hexamethylmelamine and pentamethylmelamine by liver microsomal preparations



Metabolic activation of hexamethylmelamine and pentamethylmelamine by liver microsomal preparations



Life Sciences 29(15): 1591-1598



Incubation of [14C]-ring labeled hexamethylmelamine [HMM] and pentamethylmelamine [PMM] [antitumor agents] with rat and mouse liver microsomal preparations results in metabolic activation of the 2 drugs as measured by covalent binding of radiolabel to acid-precipitable microsomal macromolecules. Covalent binding is dependent on viable microsomes, NADPH and molecular O2. Binding of HMM (280 pmol/mg protein per 15 min) was .apprx. 5 times greater than that observed for PMM (60 pmol/mg protein per 15 min) and represents 0.22% of incubated material. Similar results were found with [14C]-methyl labeled substrates. Pretreatment with phenobarbital increased covalent binding while addition of SKF 525-A, addition of glutathione or incubation in an 80% CO atmosphere reduced covalent binding.

(PDF emailed within 1 workday: $29.90)

Accession: 005879736

Download citation: RISBibTeXText

PMID: 6795407



Related references

Metabolic activation of hexa methyl melamine and penta methyl melamine by liver microsomes. Proceedings of the American Association for Cancer Research & American Society of Clinical Oncology 22: 26, 1981

Characterization of hexa methyl melamine and penta methyl melamine metabolism by rat liver microsomes and isolated hepatocytes. Pharmacologist: 215, 1980

Metabolism of hexa methyl melamine and penta methyl melamine by rat liver microsomes and isolated hepatocytes. Proceedings of the American Association for Cancer Research & American Society of Clinical Oncology 21: 257, 1980

Experimental studies on tri methyltrimethylol melamine as an alternative to hexa methyl melamine and penta methyl melamine. British Journal Of Cancer: 281-282, 1981

Determination of penta methyl melamine and hexa methyl melamine in plasma and urine by nitrogen phosphorus gas liquid chromatography. Journal of Chromatography 174(1): 245-249, 1979

Randomized phase ii trial of hexa methyl melamine vs penta methyl melamine in carcinoma of the bilharzial bladder. 1984

Comparative pharmacology of penta methyl melamine and hexa methyl melamine in mice. Cancer Research 40(8 PART 1): 2762-2767, 1980

Bio transformations of a series of methyl melamine homologues of hexa methyl melamine in vivo. Proceedings of the American Association for Cancer Research 15: 15, 1974

Effect of microsomal enzyme inducing chemicals on the metabolism of hexa methyl melamine nsc 13875 in rats and hamsters. Proceedings of the American Association for Cancer Research 13: 41, 1972

Comparative kinetic evaluation of the metabolic n demethylation of hexa methyl melamine and its metabolites in vitro. British Journal of Cancer 43(5): 730-731, 1981

Synthesis of tetra methyl carbon 14 labeled penta methyl melamine 6 a new anti tumor agent. Journal Of Labelled Compounds & Radiopharmaceuticals: 779-784, 1983

Useful new combinations of hexa methyl melamine 5 fluoro uracil infusion and mitomycin c or methyl 1 2 chloroethyl 3 cyclohexyl 1 nitroso urea. Clinical Research: 431a, 1978

Penta methyl melamine hydro chloride. Drugs of the Future 4(6): 434-437, 1979

Phase 1 study of penta methyl melamine. Cancer Treatment Reports 64(12): 1319-1322, 1980

In vivo studies with hexa methyl melamine. European Journal of Cancer 14(16): 713-720, 1978