ST1936 oxalate 

ST1936 oxalate 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 oxalate also shows moderate affinity (K_i of 300 nM) for human and rat α2 adrenergic receptor^[1].

ST1936 oxalate 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 oxalate 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 oxalate reduces the frequency of spontaneous excitatory postsynaptic currents, with an IC₅₀ of 1.3 μM^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ST1936 (5, 10, 20 mg/kg; i.p.) oxalate increases in a dose dependent manner extracellular dopamine (DA) and NA levels in the prefrontal cortex (PFCX)^[2].
ST1936 (5, 10, 20 mg/kg; i.p.) oxalate 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^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

326.78

C₁₅H₁₉ClN₂O₄

1782228-83-4

CC(N1)=C(CCN(C)C)C2=C1C=CC(Cl)=C2.O=C(O)C(O)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Borsini F, et al. Effects of ST1936, a selective serotonin-6 agonist, on electrical activity of putative mesencephalic dopaminergic neurons in the rat brain. J Psychopharmacol. 2015 Jul;29(7):802-11.  [Content Brief]

  [2]. Riccioni T, et al. ST1936 stimulates cAMP, Ca2+, ERK1/2 and Fyn kinase through a full activation of cloned human 5-HT6 receptors. Eur J Pharmacol. 2011;661(1-3):8-14.  [Content Brief]

  [3]. Tassone A, et al. Activation of 5-HT6 receptors inhibits corticostriatal glutamatergic transmission. Neuropharmacology. 2011;61(4):632-637.  [Content Brief]

  [4]. Valentini V, et al. A microdialysis study of ST1936, a novel 5-HT6 receptor agonist. Neuropharmacology. 2011;60(4):602-608.  [Content Brief]