Overview
- Fukuda, T. et al. (1991) Eur. J. Pharmacol. 196, 299.
Alomone Labs Azasetron blocks 5-HT3A receptors expressed in HEK 293T cells.5-HT3A receptor currents were elicited with 10 µM 5-HT delivered every 3 minutes. Azasetron (#A-240) was applied 30 seconds before stimulation at 0.5, 1 and 20 nM, as indicated, and inhibited the 5-HT-induced current in a dose-dependent and reversible manner.
Azasetron is a potent and selective 5-HT3 receptor antagonist. It antagonizes the channel by binding to 5-HT3 receptors thereby blocking the serotonin binding site and antagonizing the indirect sympathomimetic responses to 5-HT3.
The compound is classified as a derivative of benzamide with a longer duration of action and higher affinity than other 5-HT3 receptor antagonists.
Azasetron is highly effective in preventing postoperative and chemotherapy-induced nausea and vomiting induced by anticancer drugs and radiotherapy1,2. Therefore, in most cases 5-HT3 receptor antagonists are co-administered with anticancer drugs3.
The 5-HT3 receptor subtype is a member of the cys-loop ligand-gated cation channels expressed throughout the central and peripheral nervous systems and mediate a variety of important physiological functions4.
