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ST1936 oxalate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ST1936 oxalate图片
CAS NO:1782228-83-4
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
ST1936 oxalate 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 oxalate 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)。
生物活性

ST1936 oxalate is a selective, nanomolar affinity5-HT6receptoragonist withKivalues of 13 nM, 168 nM and 245 nM for human5-HT6, 5-HT7and 5-HT2Breceptors, respectively. ST1936 oxalate also shows moderate affinity (Kiof 300 nM) for human and ratα2adrenergic receptor[1].

IC50& Target[1]

5-HT6Receptor

13 nM (Ki)

Human 5-HT7Receptor

168 nM (Ki)

5-HT2BReceptor

245 nM (Ki)

α1-adrenergic receptor

390 nM (Ki, rat)

α2-adrenergic receptor

300 nM (Ki, rat)

α2-adrenergic receptor

300 nM (Ki, human)

体外研究
(In Vitro)

ST1936 oxalate appears to be relatively selective for 5-HT6receptors, although it has shown affinity also for 5-HT2B, 5-HT1A, 5-HT7receptor 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 oxalate behaves as a full 5-HT6agonist 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 oxalate reduces the frequency of spontaneous excitatory postsynaptic currents, with an IC50of 1.3 μM[3].

体内研究
(In Vivo)

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)[2].
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[2].

分子量

326.78

Formula

C15H19ClN2O4

CAS 号

1782228-83-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.