1171123-46-8

1171123-46-8 structure

Name: EMD 386088 hydrochloride
Chemical Name: 5-chloro-2-methyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole,hydrochloride
CAS Number: 1171123-46-8
Molecular Formula: C₁₄H₁₆Cl₂N₂
Molecular Weight: 283.19600
Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
Create Date: 2016-08-24 07:58:21
Modify Date: 2024-01-08 14:19:45
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].

Name	5-chloro-2-methyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole,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

Symbol	GHS06
Signal Word	Danger
Hazard Statements	H301
Precautionary Statements	P301 + P310
RIDADR	UN 2811 6.1 / PGIII

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