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Chemical Compound Review

Azasetron     N-(1-azabicyclo[2.2.2]oct-8- yl)-4-chloro-7...

Synonyms: Nazasetron, SureCN17190, CHEMBL1598608, ANW-56613, BPBio1_001397, ...
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Disease relevance of Nazasetron


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


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


Analytical, diagnostic and therapeutic context of Nazasetron


  1. The function of 5-HT3 receptors on colonic transit in rats. Haga, K., Asano, K., Fukuda, T., Kobayakawa, T. Obes. Res. (1995) [Pubmed]
  2. Nonlinear intestinal absorption of 5-hydroxytryptamine receptor antagonist caused by absorptive and secretory transporters. Tamai, I., Saheki, A., Saitoh, R., Sai, Y., Yamada, I., Tsuji, A. J. Pharmacol. Exp. Ther. (1997) [Pubmed]
  3. High affinity binding of azasetron hydrochloride to 5-hydroxytryptamine3 receptors in the small intestine of rats. Katayama, K., Asano, K., Haga, K., Fukuda, T. Jpn. J. Pharmacol. (1997) [Pubmed]
  4. Absorption characteristics of azasetron from rectal and oral routes in rabbits. Moriyama, Y., Arimori, K., Nakano, M. Biol. Pharm. Bull. (1997) [Pubmed]
  5. Effects of ondansetron, granisetron, ramosetron, and azasetron on human neutrophil functions. Mikawa, K., Akamatsu, H., Nishina, K., Shiga, M., Niwa, Y. Gynecol. Obstet. Invest. (2002) [Pubmed]
  6. Involvement of 5-hydroxytryptamine (5-HT)3 receptor mechanisms in regulation of basal pancreatic secretion in conscious rats. Masuda, M., Miyasaka, K., Funakoshi, A. J. Auton. Nerv. Syst. (1997) [Pubmed]
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