Overview
- Abi-Dargham, A. et al. (1993) J. Neurochem. 60, 730.
Alomone Labs LY278584 blocks 5-HT3A receptors expressed in HEK 293T cells.5-HT3A receptor currents were elicited by 10 µM 5-HT, delivered every 3 minutes. LY278584 (#L-180) applied 30 seconds before stimulation at 100 nM, inhibited the 5-HT induced current in a dose dependent and reversible manner.
LY278584 is a potent and selective antagonist of 5-HT3 receptors. Its structure is very similar to granisetron, also a 5-HT3 receptor antagonist. LY278584 is a useful ligand for studying the localization of 5-HT3 receptors in rat brain1,2.
Numerous studies have shown that 5-HT3 antagonism is able to modulate mesolimbic dopaminergic activity in rodents. There is evidence that blockade of 5-HT3 receptors may be involved in nociception. Another study conducted on 5-HT3 antagonism showed that LY278584 significantly inhibits high frequency electroacupuncture antinociception in early stages3.
The 5-HT3 receptors mediate the action of serotonin in the body. These receptors are members of the Cys-loop ligand-gated cation channels, which are expressed throughout the central and peripheral nervous systems and mediate a variety of physiological functions such as emotion, cognition, memory, pain perception, and gastrointestinal functions including secretion and motility4.
