Overview
- Fukuda, T. et al. (1991) Eur. J. Pharmacol. 196, 299.
Alomone Labs Azasetron hydrochloride blocks 5-HT3A receptors expressed in HEK 293T cells.Currents were elicited by 10 µM 5-HT delivered every 3 minutes. Azasetron hydrochloride (#Y-100) was applied 30 seconds before stimulation at 1, 10 and 100 nM, as indicated, and inhibited the 5-HT-induced current in a dose-dependent and reversible manner.
Azasetron hydrochloride (Y-25130 hydrochloride) is a potent 5-HT3 receptor antagonist. It selectively and competitively binds 5-HT3 receptors thereby blocking the serotonin binding site. Azasetron is classified as a derivative of benzamide. It has a different chemical structure from other 5-HT3 receptor blockers. The significant difference is found in the pharmacokinetic profiles resulting in a longer duration of action and a higher affinity for the 5-HT3 receptor1,2. Azasetron has an IC50 value ~4.9x10-10 M4 and half life of 5.4 hours3.
The 5-HT3 receptor subtype is a member of the Cys-loop ligand-gated cation channels which are expressed throughout the central and peripheral nervous systems and mediate a variety of physiological functions5.
Azasetron is mostly administered orally and by I.V (60-70%) and excreted in the urine in an unmetabolized form. Orally-administered azasetron is shown to be absorbed and secreted by the saturable transport mechanism in the small intestine, resulting in good bioavailability (approximately 90%)2.
5-HT3 receptor antagonists have been established in a number of clinical trials as effective agents in the management and prevention of nausea and vomiting caused by cancer chemotherapy as well as postoperative nausea and emesis after anesthesia and surgery1,3.
