| Identification | Back Directory | [Name]
ST1936 oxalate | [CAS]
1782228-83-4 | [Synonyms]
phosphorylation,Beta Receptor,5-HT6 receptor subtype,Adrenergic Receptor,ST-1936,ST1936,ST1936 oxalate,prefrontal cortex,Inhibitor,ST 1936,5-hydroxytryptamine Receptor,5-HT Receptor,ST-1936 oxalate,Fyn,Serotonin Receptor,inhibit,neurons | [Molecular Formula]
C15H19ClN2O4 | [MOL File]
1782228-83-4.mol | [Molecular Weight]
326.78 |
| Hazard Information | Back Directory | [Uses]
ST1936 oxalate is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 oxalate also shows moderate affinity (Ki of 300 nM) for human and rat α2 adrenergic receptor[1]. | [in vivo]
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]. | [IC 50]
5-HT6 Receptor: 13 nM (Ki); Human 5-HT7 Receptor: 168 nM (Ki); 5-HT2B Receptor: 245 nM (Ki); α1-adrenergic receptor: 390 nM (Ki, rat); α2-adrenergic receptor: 300 nM (Ki, rat); α2-adrenergic receptor: 300 nM (Ki, human) | [References]
[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. DOI:10.1177/0269881115573804
[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. DOI:10.1016/j.ejphar.2011.04.028
[3] Tassone A, et al. Activation of 5-HT6 receptors inhibits corticostriatal glutamatergic transmission. Neuropharmacology. 2011;61(4):632-637. DOI:10.1016/j.neuropharm.2011.05.004
[4] Valentini V, et al. A microdialysis study of ST1936, a novel 5-HT6 receptor agonist. Neuropharmacology. 2011;60(4):602-608. DOI:10.1016/j.neuropharm.2010.12.006 |
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