SB-207266

SB-207266 (CAS No.: 152811-62-6) is a potent and selective antagonist of the serotonin 5-HT4 receptor, belonging to the indole derivative class and widely utilized as a pharmacological tool in studies of serotonergic signaling. It exhibits high affinity for human 5-HT4 receptors, with binding activity in the subnanomolar range, and acts through competitive inhibition to block receptor activation and downstream signaling, including suppression of cAMP production in cellular systems. In vitro, SB-207266 effectively attenuates 5-HT-induced responses in recombinant cell lines and native tissues, while in vivo studies demonstrate its ability to inhibit serotonin-mediated physiological processes such as intestinal peristalsis and bladder detrusor muscle contraction. These properties make it particularly valuable for investigating the role of 5-HT4 receptors in gastrointestinal motility, urinary function, and cardiovascular regulation. SB-207266 has been applied in both cell-based assays and animal models to explore mechanisms underlying disorders such as overactive bladder and heart failure, as well as for target validation and drug discovery efforts focused on serotonergic modulation, with experimental concentrations or dosing regimens varying according to specific study designs.