EMD 386088 hydrochloride

[Description]:

EMD386088 is a potent serotonin 6 receptor (5-HT6R) agonist. EMD386088 induces cell death. EMD386088 regulates the activity of ERK1/2. EMD386088 has the potential for the research of alzheimer's disease (AD) and schizophrenia[1][2][3].

[Related Catalog]:

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[Target]

5-HT6 Receptor

[In Vitro]

EMD386088 (1, 10, 60 μM; 0-18 h) induces cell death in a dose- and time- dependent manner[1]. EMD386088 (1, 10, 60 μM) regulates the activity of ERK1/2 in a 5-HT6R-dependent and 5-HT6R–independent manner[1]. Cell Viability Assay[1] Cell Line: HEK/HA-5-HT6R, native HEK293 cells Concentration: 1, 10, 60 μM Incubation Time: 0-18 h Result: Induced cell death in HEK293 cells stably expressing HA-5-HT6R (HEK/HA-5-HT6R) and in native HEK293 cells in a dose- and time- dependent manner. Western Blot Analysis[1] Cell Line: HEK/HA-5-HT6R, native HEK293 cells Concentration: 1, 10, 60 μM Incubation Time: 0-18 h Result: Led to the activation of ERK1/2 at 0-30 μM, retarded ERK1/2 activation at a high dose of 60 μM in HEK/HA-5-HT6R cells.

[In Vivo]

EMD386088 (1, 5, 10 mg/kg) impairs both short-term memory (STM) and long-term memory (LTM) at 5 mg/kg, but produces no significant effects at 10 mg/kg in male Wistar rats[2]. EMD386088 (0, 2, 4 mg/kg) significantly impairs spontaneous alternation performancein at 2 mg/kg, but the high dose of 4 mg/kg dose not reach significance in C57BL/6J mice[3].

[References]

[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.

[ Molecular Formula ]:
C₁₄H₁₆Cl₂N₂

[ Molecular Weight ]:
283.19600

[ Exact Mass ]:
282.06900

[ PSA ]:
27.82000

[ LogP ]:
4.63720

Click to get detail MSDS

[ Symbol ]:

GHS06

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H301

[ Precautionary Statements ]:
P301 + P310

[ RIDADR ]:
UN 2811 6.1 / PGIII

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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