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EMD 386088 hydrochloride

EMD 386088 hydrochloride用途

EMD386088是一种有效的5-羟色胺6受体(5-HT6R)激动剂。EMD386088诱导细胞死亡。EMD386088调节ERK1/2的活性。EMD3860 88具有研究阿尔茨海默病(AD)和精神分裂症的潜力[1][2][3]。

EMD 386088 hydrochloride名称

[ CAS 号 ]:
1171123-46-8

[ 英文名 ]:
EMD 386088 hydrochloride

EMD 386088 hydrochloride生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 神经疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体

信号通路 >> 神经信号通路 >> 5-HT受体

[ 靶点 ]

5-HT6 Receptor

[体外研究]

EMD386088(1,10,60μM；0-18小时)以剂量和时间依赖性方式诱导细胞死亡[1]。EMD386088(1,10,60μM)以5-HT6R依赖性和5-HT6AR非依赖性的方式调节ERK1/2的活性[1]。细胞活力测定[1]细胞系：HEK/HA-5-HT6R,天然HEK293细胞浓度：1、10、60μM孵育时间：0-18小时结果：在稳定表达HA-5-HT6R的HEK293(HEK/HA-5-HT6R)细胞和天然HEK2 93细胞中以剂量和时间依赖性方式诱导细胞死亡。Western Blot分析[1]细胞系：HEK/HA-5-HT6R,天然HEK293细胞浓度：1,10,60μM孵育时间：0-18小时结果：导致ERK1/2在0-30μM时激活,在高剂量60μM时,在HEK/HA-5-HT6R细胞中延迟ERK1/2激活。

[体内研究]

EMD386088(1,5,10 mg/kg)在5 mg/kg时损害短期记忆(STM)和长期记忆(LTM),但在10 mg/千克时对雄性Wistar大鼠没有显著影响[2]。EMD386088(0、2、4 mg/kg)在2 mg/kg时显著损害了自发的交替表现,但高剂量的4 在C57BL/6J小鼠中,mg/kg剂量未达到显著水平[3]。

[参考文献]

[1]. Yun HM, et al. 5-HT6 receptor ligands, EMD386088 and SB258585, differentially regulate 5-HT6 receptor-independent events. Toxicol In Vitro. 2011 Dec;25(8):2035-40.

[2]. Meneses A, et al. The effects of the 5-HT(6) receptor agonist EMD and the 5-HT(7) receptor agonist AS19 on memory formation. Behav Brain Res. 2008 Dec 16;195(1):112-9.

[3]. Amodeo DA, et al. 5-HT6 receptor agonist EMD386088 impairs behavioral flexibility and working memory. Behav Brain Res. 2018 Sep 3;349:8-15.

EMD 386088 hydrochloride物理化学性质

[ 分子式 ]:
C₁₄H₁₆Cl₂N₂

[ 分子量 ]:
283.19600

[ 精确质量 ]:
282.06900

[ PSA ]:
27.82000

[ LogP ]:
4.63720

EMD 386088 hydrochlorideMSDS

详细MSDS(安全技术说明书)

EMD 386088 hydrochloride安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301

[ 警示性声明 ]:
P301 + P310

[ 危险品运输编码 ]:
UN 2811 6.1 / PGIII

EMD 386088 hydrochloride文献

Excess of serotonin affects neocortical pyramidal neuron migration.

Transl. Psychiatry 1 , e47, (2011)

The serotonin transporter (SERT) is a key molecule involved in the homeostasis of extracellular levels of serotonin and is regulated developmentally. Genetic deletion of SERT in rodents increases extr...

5-HT(6) receptor agonists and antagonists enhance learning and memory in a conditioned emotion response paradigm by modulation of cholinergic and glutamatergic mechanisms.

Br. J. Pharmacol. 167(2) , 436-49, (2012)

5-HT(6) receptors are abundant in the hippocampus, nucleus accumbens and striatum, supporting their role in learning and memory. Selective 5-HT(6) receptor antagonists produce pro-cognitive effects in...

The 5-HT6 receptor agonist EMD 386088 produces antidepressant and anxiolytic effects in rats after intrahippocampal administration.

Psychopharmacology 217(3) , 411-8, (2011)

Preclinical data suggest a possible role for 5-HT6 receptors in depression and anxiety. However, the results of pharmacological studies are equivocal since both blockade and stimulation of 5-HT6 recep...

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