Disease relevance of Nazasetron

• Azasetron may improve bowel function in stress-related colonic dysfunction like irritable bowel syndrome [1].
• The mechanism of the nonlinear concentration dependence of intestinal absorption of the 5-hydroxytryptamine receptor antagonist azasetron was studied by use of rat in situ intestinal perfusion, as well as an in vitro Ussing-type chamber method mounted with rat intestinal tissue and cultured monolayers of human adenocarcinoma Caco-2 cells [2].
• Azasetron has a high affinity for 5-HT3 receptor in the gastrointestinal organ, the very site of its antiemetic action against chemotherapy-induced emesis [3].

High impact information on Nazasetron

• When the initial uptake rate of azasetron by Caco-2 cells was measured, it was saturable with an apparent half-saturation concentration of 15 mM and was reduced in the presence of several cationic compounds [2].
• The intestinal absorption rate constant of azasetron evaluated by the Doluisio method increased significantly with increasing concentration of azasetron up to 10 mM in a nonlinear fashion and tended to decrease at higher concentrations [2].
• Furthermore, the multidrug-resistant cancer cell line K562/ADM that overexpresses P-glycoprotein accumulated azasetron less extensively than did the parental drug-sensitive K562 cells [2].
• These observations suggest that azasetron is taken up by a carrier-mediated transport mechanism across the intestinal epithelial cells [2].
• A potent and selective 5-HT3 receptor antagonist, azasetron (+/-)-N-(1-azabicyclo[2.2.2]oct-3-yl)-6-chloro- 4-methyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazine-8-carboxamide monohydrochloride ; 0.01-10 mg/kg, p.o.¿ inhibited the 5-HT-, CRF- and stress-accelerated colonic transit in a dose-dependent manner [1].

Chemical compound and disease context of Nazasetron

• Consequently, the suppository form of azasetron hydrochloride may be feasible for the treatment of chemotherapy-induced acute emesis and nausea [4].

Biological context of Nazasetron

• We conclude that intestinal transport of azasetron involves specialized transporters in both the absorptive and secretory directions, and the complex nonlinear intestinal absorption characteristics can be ascribed to the participation of multiple transport mechanisms [2].

Anatomical context of Nazasetron

• Effects of ondansetron, granisetron, ramosetron, and azasetron on human neutrophil functions [5].

Analytical, diagnostic and therapeutic context of Nazasetron

• Intravenous injection of azasetron significantly increased pancreatic fluid and protein outputs in a dose-dependent manner [6].
• The serum concentrations of azasetron following rectal administration as a suppository increased rapidly and showed the mean tmax value of 0.18 h [4].

References