In vitro and in vivo mechanistic studies toward understanding the role of 1-aminobenzotriazole in rat drug-drug interactions was written by Boily, Marc-Olivier;Chauret, Nathalie;Laterreur, Julie;Leblond, Francois A.;Boudreau, Chantal;Duquet, Marie-Claude;Levesque, Jean-Francois;Ste-Marie, Line;Pichette, Vincent. And the article was included in Drug Metabolism & Disposition in 2015.Formula: C6H6N4 This article mentions the following:
1-Aminobenzotriazole (ABT) is regularly used in vivo as a nonspecific and irreversible cytochrome P 450 inhibitor to elucidate the role of metabolism on the pharmacokinetic profile of xenobiotics. However, few reports have considered the recent findings that ABT can alter drug absorption or have investigated the possible differential inhibition of ABT on intestinal and hepatic metabolism To address these uncertainties, pharmacokinetic studies under well controlled and defined ABT pretreatment conditions (50 mg/kg, 1 h ABT i.v. and 16 h ABT p.o.)were conducted prior to the oral administration of metoprolol, a permeable P 450 probe that undergoes extensive intestinal and hepatic metabolism The pharmacokinetic profile of metoprolol was affected differently by the two ABT pretreatments. An increase in area under the curve of 16-fold with ABT p.o. and 6.5-fold with ABT i.v. was observed compared with control. Based on in vitro studies, this difference could not be attributed to a differential inhibition of intestinal and hepatic metabolism In the ABT i.v. pretreatment group, the increase in area under the curve was also associated with a prolonged time at maximal concentration (24-fold vs. control), suggesting a delay in absorption. This was further confirmed by the administration of a charcoal meal, which resulted in a 7-fold increase in stomach weights in the 1-h ABT pretreated groups compared with the untreated or 16-h ABT pretreated rats. Based on these results,we recommend pretreating rats with ABT p.o. 16 h before the administration of a test compound to preserve the inhibitory effect on intestinal and hepatic metabolism and avoid the confounding effect on drug absorption. In the experiment, the researchers used many compounds, for example, 1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6Formula: C6H6N4).
1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6) belongs to triazole derivatives. However, triazoles are also useful in bioorthogonal chemistry, because the large number of nitrogen atoms causes triazoles to react similar to azides. Due to the structural characteristics, both 1,2,3- and 1,2,4-triazoles are able to accommodate a broad range of substituents (electrophiles and nucleophiles) around the core structures and pave the way for the construction of diverse novel bioactive molecules.Formula: C6H6N4
Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics