ST1936

ST1936 is a selective, nanomolar affinity 5-HT₆ receptor agonist with K_i values of 13 nM, 168 nM and 245 nM for human 5-HT₆, 5-HT₇ and 5-HT_2B receptors, respectively. ST1936 also shows moderate affinity (K_i of 300 nM) for human and rat α2 adrenergic receptor^[1]. In Vitro: ST1936 appears to be relatively selective for 5-HT₆ receptors, although it has shown affinity also for 5-HT_2B, 5-HT_1A, 5-HT₇ receptor and α-adrenergic receptors when tested in a broad crossreactivity panel that comprised G-protein-coupled receptors, ion channel binding sites, enzymes, and transporters^[1].
ST1936 behaves as a full 5-HT₆ agonist on cloned cells and is able to increase Ca²⁺ concentration, phosphorylation of Fyn kinase, and regulate the activation of ERK1/2 that is a downstream target of Fyn kinase^[2].
ST1936 reduces the frequency of spontaneous excitatory postsynaptic currents, with an IC₅₀ of 1.3 μM^[3]. In Vivo: ST1936 (5, 10, 20 mg/kg; i.p.) increases in a dose dependent manner extracellular dopamine (DA) and NA levels in the prefrontal cortex (PFCX)^[4].
ST1936 (5, 10, 20 mg/kg; i.p.) increases extracellular DA and NA levels in the nucleus accumbens (NAc) core. Doses of 10 mg/kg increases dialysate DA (peak: 179%) while higher dose increases both DA and NA dialysates (201% and 231%, respectively). Doses of 5 mg/kg does not produce any effect^[4].