(R,S)-CHPG

Names

[ Name ]:
(R,S)-CHPG

[Synonym ]:
Pregnanolone
CHPG
2-chloro-5-hydroxyphenylglycine

Biological Activity

[Description]:

CHPG is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells[1]. CHPG protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways[2].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Signaling Pathways >> PI3K/Akt/mTOR >> Akt

Research Areas >> Inflammation/Immunology

Signaling Pathways >> GPCR/G Protein >> mGluR

Signaling Pathways >> MAPK/ERK Pathway >> ERK

Signaling Pathways >> Stem Cell/Wnt >> ERK

[Target]

mGluR5

NF-κB

ERK

Akt

[In Vitro]

CHPG (10-500 µM; 24 hours) significantly increases the cell viability and decreases the LDH release after SO2 derivatives treatment[1]. CHPG (0.5 mM; 30 mins ) protects BV2 cells against SO2-induced apoptosis[1]. CHPG (0.5 mM; 30 mins) treatment alone increases the expression of TSG-6 in both mRNA and protein levels[1]. Cell Viability Assay[1] Cell Line: BV2 microglial cells Concentration: 10, 50, 100 and 500 µM Incubation Time: 24 hours Result: Increased the cell viability. Apoptosis Analysis[1] Cell Line: BV2 microglial cells Concentration: 0.5 mM Incubation Time: 30 mins Result: Protected BV2 cells against SO2-induced apoptosis. Western Blot Analysis[1] Cell Line: BV2 microglial cells Concentration: 0.5 mM Incubation Time: 30 mins Result: Increased the expression of TSG-6 in both mRNA and protein levels.

[In Vivo]

CHPG (injection; 250 nM; for 7 days) reduces significantly cerebral lesion volume[2]. Animal Model: Adult Sprague-Dawley male rats weighing 280-320 g[2] Dosage: 250 nM Administration: Injection; for 7 days Result: Reduced significantly cerebral lesion volume.

[References]

[1]. Qiu JL, et al. The selective mGluR5 agonist CHPG attenuates SO₂-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells. Neurochem Int. 2015 Jun-Jul;85-86:46-52.

[2]. Chen T, et al. The selective mGluR5 agonist CHPG protects against traumatic brain injury in vitro and in vivo via ERK and Akt pathway. Int J Mol Med. 2012 Apr;29(4):630-6.

Chemical & Physical Properties

[ Molecular Formula ]:
C₈H₈ClNO₃

[ Molecular Weight ]:
201.60700

[ Exact Mass ]:
201.01900

[ PSA ]:
83.55000

[ LogP ]:
1.83030

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H315-H319-H335

[ Precautionary Statements ]:
P261-P305 + P351 + P338

[ Personal Protective Equipment ]:
dust mask type N95 (US);Eyeshields;Gloves

[ Hazard Codes ]:
Xi

[ Risk Phrases ]:
R36/37/38

[ Safety Phrases ]:
S26

[ RIDADR ]:
NONH for all modes of transport

Articles

mGluR5 in the nucleus accumbens shell regulates morphine-associated contextual memory through reactive oxygen species signaling.

Addict. Biol. 20 , 927-40, (2015)

Emerging evidence indicates that metabotropic glutamate receptor 5 (mGluR5) critically modulates drug and drug-related behaviors. However, the role of mGluR5 in the opiate-induced contextual memory re...

Modulatory effects of activation of metabotropic glutamate receptors on GABAergic circuits in the mouse thalamus.

J. Neurophysiol. 113 , 2646-52, (2015)

Metabotropic glutamate receptors (mGluRs) are widely distributed in the central nervous system and modulate the release of neurotransmitters in different ways. We have previously shown that activation...

Stimulation-evoked Ca2+ signals in astrocytic processes at hippocampal CA3-CA1 synapses of adult mice are modulated by glutamate and ATP.

J. Neurosci. 35(7) , 3016-21, (2015)

To date, it has been difficult to reveal physiological Ca(2+) events occurring within the fine astrocytic processes of mature animals. The objective of the study was to explore whether neuronal activi...

Related Compounds

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