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Chemical Structure| 96206-92-7 Chemical Structure| 96206-92-7

Structure of MPEP
CAS No.: 96206-92-7

Chemical Structure| 96206-92-7

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MPEP is a potent and highly selective non-competitive antagonist at the mGlu5 receptor subtype (IC50 = 36 nM) and a positive allosteric modulator at mGlu4 receptors.

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Product Details of MPEP

CAS No. :96206-92-7
Formula : C14H11N
M.W : 193.24
SMILES Code : CC1=NC(C#CC2=CC=CC=C2)=CC=C1
MDL No. :MFCD03787983
InChI Key :NEWKHUASLBMWRE-UHFFFAOYSA-N
Pubchem ID :3025961

Safety of MPEP

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of MPEP

GPCR

Isoform Comparison

Biological Activity

Target
  • mGluR5

    mGluR5, IC50:36 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Dopamine neurons 300 nM Block mGluR5 receptors to prevent cocaine-induced reduction in mGluR1 currents Neuropsychopharmacology. 2015 Sep;40(10):2418-24
MN9D cells 100 μM 30 min Inhibited rotenone-induced JNK phosphorylation, protected cells from apoptosis Neurotherapeutics. 2019 Jul;16(3):761-783
C6 astroglial cells 10 μM 25 min Blocked mGluR5 activity, inhibited DHPG-induced AKT and ERK1/2 phosphorylation Neurotherapeutics. 2019 Jul;16(3):761-783
Hippocampal organotypic slice cultures (HOCS) 36 nM 21–45 days MPEP significantly ameliorated the neurodegeneration triggered by prion infection PLoS Pathog. 2017 Nov 27;13(11):e1006733
Cerebellar organotypic slice cultures (COCS) 10 nM 21–45 days MPEP significantly ameliorated the neurodegeneration triggered by prion infection PLoS Pathog. 2017 Nov 27;13(11):e1006733
Jurkat E6.1 cells 20 μM 20 minutes To investigate the effect of MPEP on mGluR5 activity in Jurkat cells, results showed that MPEP pretreatment decreased RANTES release. Transl Psychiatry. 2018 May 30;8(1):110

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Wild-type and p11 knockout mice Intraperitoneal injection 3 mg/kg Single dose, behavioral tests conducted 30 min or 24 hr after administration To investigate the antidepressant-like behavioral effects of MPEP, it was found that MPEP exhibited antidepressant-like behaviors in wild-type mice, but this effect was abolished in p11 knockout mice. Mol Psychiatry. 2015 Dec;20(12):1546-56
Mice Neuropathic pain model (SNI model) Subcutaneous injection 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg Single or multiple doses, lasting for 8 days To evaluate the analgesic effects and side effects of MPEP in a neuropathic pain model. Results showed that MPEP partially alleviated mechanical hyperalgesia early (10 days) but had reduced efficacy late (30 days). Additionally, MPEP did not exhibit the side effects of traditional opioids, such as respiratory depression and locomotor behavior changes. Pain. 2020 Sep 1;161(9):2041-2057
Wistar rats Chronic migraine rat model Intracerebroventricular administration 0.2 μg, 2 μg, 5 μg/5 μL Single administration MPEP alleviated the allodynia and reduced the expression of CGRP, pCREB-S133, c-Fos, PSD, Syp and Syt-1 and synaptic transmission in CM rats. Moreover, the administration of MPEP inhibited the upregulation of PKC and pNR2B-Y1472. J Headache Pain. 2020 Dec 4;21(1):139
Mice Intraperitoneal injection 30 mg/kg Single injection Block mGluR5 receptors to prevent cocaine-induced reduction in mGluR1 currents Neuropsychopharmacology. 2015 Sep;40(10):2418-24
ICR-CD1 mice Neuropathic pain model Intrathecal injection 1, 3, 10 nmol 30-minute intervals To evaluate the synergistic effects of MPEP with morphine-like drugs, results showed that MPEP combined with oxymorphone or oxymorphamine had synergistic analgesic effects. Pain. 2017 Dec;158(12):2431-2441
Sprague-Dawley rats Rotenone-induced PD model Intraperitoneal injection 1.5 mg/kg/day For continuous 3 weeks MPEP attenuated behavioral deficits and dopaminergic neuronal death, while CAL knockdown weakened the protective effect of MPEP Neurotherapeutics. 2019 Jul;16(3):761-783
C57BL/6J male mice Prion-infected mouse model Oral 30 mg/kg/day Daily until the end of the experiment MPEP significantly delayed the onset of motor deficits and moderately prolonged survival of prion-infected mice PLoS Pathog. 2017 Nov 27;13(11):e1006733
Cynomolgus monkeys (Macaca fascicularis) MPTP-induced Parkinson's disease model Oral 10 mg/kg Once daily for one month MPEP blockade of metabotropic glutamate receptor 5 prevents L-Dopa-induced dyskinesias and is associated with reduced inflammation in the brain of Parkinsonian monkeys. MPEP co-treatment with L-Dopa significantly reduced the development of dyskinesias and decreased levels of inflammatory markers (Iba1, CD68, and GFAP) in the basal ganglia. Cells. 2022 Feb 16;11(4):691

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01024491 Premature Ejaculation Phase 3 Completed - Mexico ... More >> Asociacion Mexicana para la Salud Sexual, A.C. Mexico City, Mexico D.F., Mexico, 14000 Centro Especializado en Urología y Andrología del Hospital Star Médica Mexico City, Mexico D.F, Mexico, 06700 Less <<
NCT03506945 Depressive Symptoms ... More >> Stress, Psychological Less << Not Applicable Not yet recruiting July 2023 United States, California ... More >> University of California San Diego La Jolla, California, United States, 92093 Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

5.17mL

1.03mL

0.52mL

25.87mL

5.17mL

2.59mL

51.75mL

10.35mL

5.17mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

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
Protocol 2

References

 

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