RS-39604

RS-39604 is a potent, selective, and orally active small molecule antagonist of the serotonin 5-HT4 receptor. It exhibits high affinity for the serotonin 5-HT4 receptor (pKi = 9.1 in guinea pig striatal membranes), with over 1000-fold selectivity compared to other receptors such as 5-HT1A, 5-HT2C, 5-HT3, dopamine D1/D2, muscarinic M1/M2, angiotensin AT1/B1 and alpha adrenergic α1C receptors. The presence of a ketone group confers a relatively long half-life to the compound. RS‑39604 is suitable for *in vivo* studies due to its oral bioavailability and long-lasting action[1][3][7]. It has been used primarily as an experimental tool to investigate physiological and pathophysiological roles of the 5‑HT4 receptor in various tissues including myocardium (heart), alimentary tract (gut), and lower urinary tract[7]. There is no evidence that it has advanced beyond preclinical or early investigational stages.

Other names

Methanesulfonamide, n-(2-(4-(3-(4-amino-5-chloro-2-((3,5-dimethoxyphenyl)methoxy)phenyl)-3-oxopropyl)-1-piperidinyl)ethyl)-