ST1936

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是一种选择性的纳摩尔亲和力的 5-HT6 受体激动剂，对人 5-HT6、5-HT7 和 5-HT2B 受体的 Ki 值分别为 13 nM，168 nM 和 245 nM。ST1936对人和大鼠的 α2 肾上腺素受体也显示出中等亲和力 (Ki 为 300 nM)。

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.

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GPCR/G Protein

5-HT Receptor

5-HT Receptor

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1210-81-7

236.74

C13H17ClN2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (422.40 mM; 超声助溶 )

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

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(-20℃)

With Ice Pack

≥ 2 years