ST1936 oxalate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ST1936 草酸盐是 5-HT6 受体的选择性纳摩尔亲和力激动剂。

ST1936 oxalate is a selective, nanomolar affinity agonist of 5-HT6 receptor(Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively).

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

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).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.

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Endocrinology/Hormones

5-HT Receptor

5-HT6 Receptor|Human 5-HT7 Receptor |5-HT2B Receptor

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1782228-83-4

326.78

C15H19ClN2O4

>98% (HPLC)

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CC1=C(C2=C(N1)C=CC(=C2)Cl)CCN(C)C.C(=O)(C(=O)O)O

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(-20℃)

With Ice Pack

≥ 2 years