Overview
- Orjales, A. et al. (1997) J. Med. Chem. 40, 586.
Alomone Labs Lerisetron blocks 5-HT3A receptors expressed in HEK 293T cells.5-HT3A receptor currents were elicited by 10 µM 5-HT, delivered every 3 minutes. Lerisetron (#L-175) 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.
Lerisetron, a piperazinylbenzimidazole derivative, is a potent and highly selective blocker of serotonin 5-HT3 channels with antiemetic effects. The drug is shown to be effective in the treatment of nausea and vomiting caused by emetogenic cytotoxic drugs1,2.
Lerisetron antagonizes the serotonin action on the presynaptic 5-HT3 receptor that is implicated at the emetic reflex2,3.
The 5-HT3 receptor mediates the action of serotonin in the body. This receptor is a member of the Cys-loop ligand-gated cation channels, which are expressed throughout the central and peripheral nervous systems and mediates a variety of physiological functions such as: emotion, cognition, memory, pain perception, and gastrointestinal functions including secretion and motility4.
