ST1936

• CAT Number: I010937
• CAS Number: 1210-81-7
• Molecular Formula: C13H17ClN2
• Molecular Weight: 236.74
• Purity: ≥95%
• Synonyms: 2-(5-chloro-2-methyl-1H-indol-3-yl)-N,N-dimethylethanamine
• InChI: InChI=1S/C13H17ClN2/c1-9-11(6-7-16(2)3)12-8-10(14)4-5-13(12)15-9/h4-5,8,15H,6-7H2,1-3H3
• InChIKey: KSYMELKKLOFABL-UHFFFAOYSA-N
• SMILES: CC1=C(C2=C(N1)C=CC(=C2)Cl)CCN(C)C

ST1936 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 also shows moderate affinity (Ki of 300 nM) for human and rat α2 adrenergic receptor[1].
ST1936 appears to be relatively selective for 5-HT6 receptors, although it has shown affinity also for 5-HT2B, 5-HT1A, 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].
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].

Reference

[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.
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[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.
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[3]. Tassone A, et al. Activation of 5-HT6 receptors inhibits corticostriatal glutamatergic transmission. Neuropharmacology. 2011;61(4):632-637.
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[4]. Valentini V, et al. A microdialysis study of ST1936, a novel 5-HT6 receptor agonist. Neuropharmacology. 2011;60(4):602-608.
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