Overview
- Clark, R.D. et al. (1995) Bioorg. Med. Chem. Lett. 5, 1853.
Alomone Labs RS 56812 hydrochloride activates 5-HT3A receptors expressed in HEK 293T cells.Currents were elicited by 1, 10 or 100 nM RS 56812 hydrochloride (#R-130), as indicated. The currents that were elicited were comparable in amplitude to the cell’s response to 10 µM 5-HT (not shown here).
RS 56812 hydrochloride is a highly potent and selective 5-HT3 partial agonist with an EC50 value of 18 nM. It has been shown to bind to 5-HT3 receptors with high affinity. It has the ability to induce the von Bezold-jarisch reflex and to depolarize the rat vagus nerve1.
The affinity of RS 56812 is comparable to that of other potent full agonists. RS 56812 is thus a valuable tool for investigating the agonist interaction with the 5-HT3 receptor in electrophysiological and radioligand binding studies1.
RS 56812 exists in the R and S isomeric forms. It has been shown to improve performance in memory tests conducted on monkeys. It appears that the R isomer is more active and seems to produce more systematic and reproducible improvement in memory. RS 56812 is suggested to have a therapeutic potential in disorders involving cognitive decline2.
