Application of osmotic pumps for sustained release of 1-aminobenzotriazole and inhibition of cytochrome P450 enzymes in mice: model comparison with the hepatic P450 reductase null mouse was written by Stringer, Rowan A.;Ferreira, Suzie;Rose, Jonathan;Ronseaux, Sebastien. And the article was included in Drug Metabolism & Disposition in 2016.Recommanded Product: 1H-Benzo[d][1,2,3]triazol-1-amine This article mentions the following:
The effectiveness of controlled release 1-aminobenzotriazole (ABT) administration to inhibit cytochrome P 450 (P 450) enzymes has been evaluated in mice. To maximize the duration of P 450 inhibition in vivo, ABT was administered via an osmotic pump. The degree of P 450 inhibition was compared with that achieved with a single bolus dose of ABT. Two-hour prior s.c. treatment of mice with ABT (50 mg/kg) inhibited antipyrine clearance by 88%. A less pronounced inhibitory effect (29% reduction in clearance) was observed when ABT was administered 24-h before antipyrine administration, indicating partial restoration of P 450 activity during this longer pretreatment time. The duration of ABT in mice was very short (mean residence time = 1.7 h) after s.c. bolus administration. When the inhibitor was delivered by an osmotic pump, maximum blood concentrations of the inhibitor were observed 24 h after device implantation and were maintained at steady state for 6 days. Inhibition of P 450 activity, as measured by antipyrine clearance, was confirmed at 24 h and 120 h after pump implantation, highlighting the utility of this method as a longer term model for P 450 inhibition in mice. The magnitude of P 450 inhibition in ABT-treated mice was compared with that in hepatic P 450 reductase null mice and both models were comparable. In vivo ABT administration by an osmotic pump offers an effective approach for longer-term P 450 inhibition in mice and avoids the necessity for multiple dosing of the inhibitor. In the experiment, the researchers used many compounds, for example, 1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6Recommanded Product: 1H-Benzo[d][1,2,3]triazol-1-amine).
1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6) belongs to triazole derivatives. Triazoles consist of a five-membered ring containing three nitrogen atoms and are biologically active, especially as antifungal, antimicrobial and enzyme inhibitors. Triazoles are compounds with a vast spectrum of applications, varying from materials (polymers), agricultural chemicals, pharmaceuticals, photoactive chemicals and dyes.Recommanded Product: 1H-Benzo[d][1,2,3]triazol-1-amine
Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics