Metabolic activation of hexamethylmelamine and pentamethylmelamine (cas 16268-62-5) by liver microsomal preparations
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Add time:07/30/2019 Source:sciencedirect.com
Incubation of [14C]-ring labeled hexamethylmelamine and pentamethylmelamine (cas 16268-62-5) with rat and mouse liver microsomal preparations results in metabolic activation of both drugs as measured by covalent binding of radiolabel to acid-precipitable microsomal macromolecules. Covalent binding is dependent on viable microsomes, NADPH, and molecular oxygen. Binding of HMM (280 pmol/mg protein/15 min) was approximately 5 times greater than that observed for PMM (60 pmol/mg protein/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% carbon monoxide atmosphere reduced covalent binding.
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