ST1936 is a potent, selective 5-HT6 receptor agonist with Ki of 13 nM, >10-fold selectivity over 5-HT7 and 5-HT2B receptors. ST1936 displays moderate affinity for human α2 adrenergic receptors (Ki = 300 nM). ST1936 was shown to increase Ca2+ concentration and phosphorylation of Fyn kinase, and regulate the activation of ERK1/2 in cloned cells. ST1936 reduced the frequency of spontaneous excitatory postsynaptic currents with IC50 of 1.3 uM, inhibited corticostriatal glutamatergic transmission.
