SB-258585 is a potent, selective antagonist of the serotonin 5-HT6 receptor (pKi = 8.53). It displays over 100-fold selectivity for 5-HT6 over other 5-HT, dopamine, and α-adrenergic receptors. Radiolabeled forms of SB-258585 have been used to evaluate other potential ligands of the 5-HT6 receptor. SB-258585 has been used in cells and in animals to evaluate the role of the 5-HT6 receptor in diverse processes.
