Ro-24-4736 is primarily used in research settings as a potent and selective antagonist for the 5-HT2B receptor, a subtype of serotonin receptors. Its main application lies in studying cardiac function and valvular heart disease, as activation of 5-HT2B receptors has been linked to heart valve proliferation and fibrosis. By blocking this receptor, Ro-24-4736 helps investigate the role of serotonin signaling in cardiovascular pathologies.

It is also employed in neuroscience research to differentiate the effects of various serotonin receptor subtypes, aiding in the development of safer pharmacological agents—particularly for drugs targeting the central nervous system—where off-target activation of 5-HT2B could lead to cardiac complications. Due to its selectivity, it serves as a valuable tool compound in validating the safety profiles of new drug candidates, especially in preclinical studies.