In rat, histamine metabolism is altered by some nonspecific inhibitors of monoamine oxidase (MAO) such as iproniazid, and, to a lesser extent, tranylcypromine. Type A MAO inhibitors, such as clorgyline and MD780515, do not seem to interfere with the metabolism of histamine. Deprenyl, a type B MAO inhibitor, shows some inhibition which is, however, much lower than that observed with iproniazid. The strong effect of iproniazid is probably due to its DAO inhibiting properties.
Von den Estern (III) werden (IIIa) aus den Komponenten (I) und (II) gewonnen; (IIIb) sind bekannt, und (IIIc) werden aus dem Methylthioderivat (IV) mit entsprechenden Aminen (VI) (Methyl‐ bzw. Dimethylamin) gewonnen.
Different metabolites (2‐7) of oxapadol 1 were carried out from 3 by known methods. Their acidic hydrolysis provided compounds 4 in which the dioxolane moiety was opened. The reaction of glycerol with compounds 3 gave the dioxolane derivatives 5 which have a hydroxymethyl group and which (R = H) gave by oxidation the carboxylic acid 7. From 3 (R = H), the hydroxy acid 6 has been also prepared.
1. A number of metabolites of oxapadol were isolated from urine of rat, dog and man after administration of a single dose of 14C-labelled compound. They were identified by direct inlet mass spectrometry and chromatographic comparison with reference compounds. 2. Oxapadol was extensively metabolized and the unchanged drug was undetectable in rat or human urine; only traces were found in dog urine. Nine metabolites were identified in rat and dog urine, and six in man. 3. The routes of biotransformation were: (a) aromatic hydroxylation, mainly in the benzimidazole ring, (b) scission of the heterocyclic ring following two different pathways, and (c) a combination of the two. Regioselectivity was observed for aromatic hydroxylation, as only three of the four possible monohydroxy oxazepinobenzimidazoles could be detected.
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