ST1936

Research use only, not for human use.

ST1936 (ST 1936 oxalate) is a selective and highly potent 5-HT6 receptor agonist that inhibits human 5-HT6, 5-HT7 and 5-HT2B receptors by fully activating cloned human 5-HT6 receptors.

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.

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.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. ST1936 reduces the frequency of spontaneous excitatory postsynaptic currents, with an IC50 of 1.3 μM.

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).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.

——

GPCR/G Protein

5-HT Receptor

5-HT Receptor

——

——

1210-81-7

236.74

C13H17ClN2

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (422.40 mM; Ultrasonic )

CN(C)CCc1c(C)[nH]c2ccc(Cl)cc12

——

(-20℃)

With Ice Pack

≥ 2 years