产品
编 号：F622124
分子式：C15H19ClN2O4
分子量：326.78
分子式：C15H19ClN2O4
分子量：326.78
产品类型
规格
价格
是否有货
结构图
CAS No: 1782228-83-4
产品详情
生物活性：
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.
体内研究：
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.
体外研究：
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 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.
体内研究：
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.
体外研究：
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.
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