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- W2096850204 abstract "Benzyl-14C and N-methyl-3H labeled N-nitroso derivatives (NDT) of tripelennamine were synthesized by reacting the corresponding labeled parent drug with sodium nitrite at pH 1–2, and their covalent binding to rat liver musomes was compared with that of radiolabeled tripelennamine. The covalent binding of these substances is mediated by liver musomal cytochrome P-450 enzymes; it required an NADPH-generating system and oxygen, and was inhibited by CO:O2 (8:2). Reduced glutathione (1 mM) also inhibited the covalent binding. The covalent binding of NDT to liver musomal proteins from phenobarbital-pretreated rats was ten times greater than that of tripelennamine. A Km of 60 μM and a Vmax of 1 nmole/mg of protein/min were obtained for the covalent binding of NDT. Phenobarbital and acetone pretreatments of rats increased covalent binding of both the drug and its nitroso derivative, while pretreatment with 3-methyl-cholanthrene decreased their binding. These results suggest that chemically reactive intermediates of tripelennamine and NDT are involved in the covalent binding. Under the conditions in vitro employed, the rate of N-demethylation of NDT was lower than that of the parent drug. Moreover, the covalent binding of the N-methyl-3H labeled nitroso derivative was equivalent to that of the benzyl-14C labeled derivative. Thus, N-demethylation is not a requisite for the covalent binding of tripelennamine and its N-nitroso derivative. The mechanism of the covalent binding of the N-nitroso derivative of tripelennamine, therefore, differs from that of dimethylnitrosamine." @default.
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- W2096850204 date "1975-09-01" @default.
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- W2096850204 title "Enzymatic formation of chemically reactive metabolites of N-nitroso-desmethyl tripelennamine by a mechanism other than N-dealkylation" @default.
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- W2096850204 doi "https://doi.org/10.1016/0006-2952(75)90010-6" @default.
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