SML0139
EMD386088
≥98% (HPLC)
别名:
5-Chloro-2-methyl-3-(1,2,3,6-tetrahydro-4-pyridinyl)-1H-Indole hydrochloride, EMD-386088
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关于此项目
经验公式（希尔记法）:
C14H15ClN2 · HCl
化学文摘社编号:
分子量:
283.20
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352202
MDL number:
InChI
1S/C14H15ClN2.ClH/c1-9-14(10-4-6-16-7-5-10)12-8-11(15)2-3-13(12)17-9;/h2-4,8,16-17H,5-7H2,1H3;1H
SMILES string
Cl.Cc1[nH]c2ccc(Cl)cc2c1C3=CCNCC3
InChI key
WWSNDUWIZDYGIQ-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
yellow
solubility
DMSO: ≥16 mg/mL
storage temp.
2-8°C
Application
EMD386088 may be used to study 5-HT6-mediated cell signaling.
Biochem/physiol Actions
EMD-386088 is a potent serotonin 5-HT6-specific agonist. The IC50 for competition of LSD from 5-HT6 expressed in HEK cells is 7.4 nM, and the EC50 for stimulating cAMP production is 1 nM. EMD-386088 is inactive against other HT receptors except 5-HT3 (IC50 = 34 nM).
EMD386088 effectively reverses cholinergic and glutataminergic-induced deficits in cognitive functions. It may be a therapeutic option in improving associated learning in Alzheimer′s disease and schizophrenia. EMD386088 also exhibits anti-depressant and anxiolytic effects in rats.
Serotonin 5-HT6 agonist
signalword
Danger
hcodes
pcodes
Hazard Classifications
Acute Tox. 3 Oral
存储类别
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
S Woods et al.
British journal of pharmacology, 167(2), 436-449 (2012-05-10)
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 several learning and memory paradigms while 5-HT(6) receptor agonists have been found to enhance
Agnieszka Nikiforuk et al.
Psychopharmacology, 217(3), 411-418 (2011-04-19)
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 receptors may evoke antidepressant- and anxiolytic-like effects. In the present study, the
Magdalena Kotańska et al.
Frontiers in neuroscience, 11, 50-50 (2017-02-24)
Since 5-HT
O Riccio et al.
Translational psychiatry, 1, e47-e47 (2011-01-01)
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 extracellular levels of serotonin and affects cellular processes involved in neocortical circuit
Moritoshi Hirono et al.
Neuropharmacology, 118, 79-89 (2017-03-17)
Cerebellar Purkinje cells (PCs) project their axon collaterals to underneath of the PC layer and make GABAergic synaptic contacts with globular cells, a subgroup of Lugaro cells. GABAergic transmission derived from the PC axon collaterals is so powerful that it
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