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Chemical Structure| 219911-35-0 Chemical Structure| 219911-35-0

Structure of MPEP HCl
CAS No.: 219911-35-0

Chemical Structure| 219911-35-0

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MPEP HCl is a potent and highly selective non-competitive antagonist at the mGlu5 receptor subtype with IC50 of 36 nM.

Synonyms: MPEP (hydrochloride); MPEP Hydrochloride

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Product Details of MPEP HCl

CAS No. :219911-35-0
Formula : C14H12ClN
M.W : 229.70
SMILES Code : CC1=NC(C#CC2=CC=CC=C2)=CC=C1.[H]Cl
Synonyms :
MPEP (hydrochloride); MPEP Hydrochloride
MDL No. :MFCD02262119
InChI Key :PKDHDJBNEKXCBI-UHFFFAOYSA-N
Pubchem ID :9794588

Safety of MPEP HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of MPEP HCl

GPCR

Isoform Comparison

Biological Activity

Description
MPEP Hydrochloride is a potent, selective, noncompetitive, orally active mGlu5 receptor antagonist with an IC50 of 36 nM for inhibiting quisqualate-stimulated phosphoinositide hydrolysis. It exhibits anxiolytic and antidepressant-like effects[1][2].

In Vitro:

Cell Line
Concentration Treated Time Description References
BV-2 murine microglia cells 100 μM 24 hours MPEP increased intracellular reactive oxygen species (ROS), mitochondrial superoxide, mitochondrial mass as well as iNOS and IL-6 expression. J Neuroinflammation. 2014 Nov 19;11:190
Human corneal epithelial (HCE) cells 0.5, 0.25, 0.125, 0.0625, and 0.03125 mg/mL 48 hours To evaluate the cytotoxicity of MPEP-FK506 hydrogel on HCE cells. Results showed that 1MPEP and 2MPEP extracts exhibited lower cytotoxicity, with 2MPEP extract being the least cytotoxic. Bioact Mater. 2021 Jul 28;9:77-91

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Autism model mice (VPA-exposed) Intraperitoneal injection 10 mg/kg Single dose, 5 minutes before testing To assess the effect of MPEP on auditory evoked potentials (AEP) and prepulse inhibition (PPI) phenotypes in VPA-exposed mice. MPEP significantly reduced N1 amplitude, indicating decreased cortical excitability, but did not rescue N1 latency delays. In the frequency domain, there was a trending interactive effect of MPEP and VPA exposure on gamma PLF, boosting gamma synchrony in the VPA group while reducing gamma synchrony in SAL treated mice. Additionally, MPEP rescued PPI deficits, normalizing PPI responses in VPA-exposed mice. Biol Psychiatry. 2010 Dec 15;68(12):1100-6
Rats Alcohol-preferring (P) rats Bilateral nucleus accumbens microinjection 0 μg, 1 μg, 3 μg, 10 μg 30 minutes Microinjection of the mGluR5 antagonist MPEP in the nucleus accumbens reduced ethanol self-administration without altering locomotor activity. Biol Psychiatry. 2010 May 1;67(9):812-22
Mice FMRP-knockout mice In vitro brain slice perfusion 50 μM Single shocks or three trains of 100 Hz tetanic stimulation To investigate the effect of MPEP on LTP in the visual cortex of FMRP-knockout mice. Results showed that MPEP significantly attenuated LTP in wild-type mice but did not further alter the already reduced LTP in knockout mice, indicating the absence of mGluR5-mediated synaptic plasticity in FMRP-knockout mice. Proc Natl Acad Sci U S A. 2007 Feb 13;104(7):2454-9
Mice Fmr1 knockout mice Brain slice incubation 40 μM 1 hour MPEP failed to rescue the deficit in long-term potentiation or surface GluR1 in the amygdala of Fmr1 KO mice but reversed the decrease in mEPSC frequency. Proc Natl Acad Sci U S A. 2010 Jun 22;107(25):11591-6
Mice P11 knockout mice and mGluR5 knockout mice Intraperitoneal injection 3 mg/kg Single injection, 30 min or 24 hr prior to behavioral tests To study the antidepressant-like behavioral effects of MPEP, it was found that MPEP decreases inhibitory neuronal firing by acting on parvalbumin-positive GABAergic interneurons, leading to an increase in excitatory neuronal firing. Mol Psychiatry. 2015 Dec;20(12):1546-56

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.35mL

0.87mL

0.44mL

21.77mL

4.35mL

2.18mL

43.53mL

8.71mL

4.35mL

Dissolving Methods
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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