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    MPEP
    MPEP

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1089
    CAS #: 96206-92-7 Purity ≥98%

    Description: MPEP is a highly potent, selective, and non-competitive antagonist of mGlu5 receptor with anti-anxiolytic/antidepressant activity. It inhibits mGlu5 receptor with IC50 of 36 nM, and exhibits little activity against mGlu1b/2/3/4a/7b/8a/6 receptors. MPEP reverses maze learning and PSD-95 deficits in Fmr1 knock-out mice. Unlike the NMDA antagonist MK-801, MPEP does not injure the adult retrosplenial cortex, in which it fails to induce heat shock protein 70 (Hsp70). Moreover, MPEP does not elicit to the same extent as MK-801 apoptosis in cortical areas at perinatal stages, as revealed by caspase 3 expression. These data identify new cellular targets for the anxiolytic and antidepressant effect of MPEP, indicating also in addition that in contrast to MK-801, it lacks the cortical neurotoxicity associated with psychotomimetic side-effects. MPEP has the potential use as anxiolytic/antidepressant drug.

    References: Neuropharmacology. 1999 Oct;38(10):1493-503; Br J Pharmacol. 2001 Apr;132(7):1423-30.

    Related CAS#: 219911-35-0 (HCl)

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    Molecular Weight (MW)193.24
    FormulaC14H11N
    CAS No.96206-92-7 (free base)
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 39 mg/mL (201.8 mM) 
    Water: <1 mg/mL
    Ethanol: 39 mg/mL (201.8 mM) 
    Solubility (In vivo)2% DMSO+30% PEG 300+5% Tween 80: 10 mg/mL
    Synonyms2-methyl-6-(phenylethynyl)-pyridine; MPEP; MPEP HCl; MPEP hydrochloride


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    In Vitro

    In vitro activity: MPEP is a highly potent, selective, and non-competitive antagonist of mGlu5 receptor with IC50 of 36 nM, it exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors. MPEP reverses maze learning and PSD-95 deficits in Fmr1 knock-out mice. Unlike the NMDA antagonist MK-801, MPEP does not injure the adult retrosplenial cortex, in which it fails to induce heat shock protein 70 (Hsp70). Moreover, MPEP does not elicit to the same extent as MK-801 apoptosis in cortical areas at perinatal stages, as revealed by caspase 3 expression. These data identify new cellular targets for the anxiolytic and antidepressant effect of MPEP, indicating also in addition that in contrast to MK-801, it lacks the cortical neurotoxicity associated with psychotomimetic side-effects. MPEP has the potential use as anxiolytic/antidepressant drug. MPEP has no appreciable agonist or antagonist activity at the closely related recombinant human mGlu1b receptor expressed in CHO-K1 cells or a purinoreceptor endogenously expressed in L(tk-) cells up to concentrations of 100 μM. Furthermore, MPEP shows no appreciable agonist or antagonist activity in cAMP accumulation or [35S]-GTPγS binding assays at the recombinant human group II and III metabotropic receptors (human mGlu2, -3, -4a, -6, -7b, -8a) as well as the human NMDA (NMDAR1A/2A, -1A/2B), rat AMPA (GluR3) and human kainate (GluR6) receptor subtypes. In slices of rat neonatal hippocampus, striatum, and cortex but not cerebellum, MPEP inhibits DHPG-stimulated PI hydrolysis with IC50 of 8.0 nM, 20.5 nM, and 17.9 nM, respectively. MPEP positively modulates the hmGluR4 in a recombinant expression system, and the effect of MPEP is fully dependent on the activation of the orthosteric agonist L-AP4.


    Kinase Assay: MPEP is a highly potent, selective, and non-competitive antagonist of mGlu5 receptor with IC50 of 36 nM, it exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors.


    Cell Assay: In slices of rat neonatal hippocampus, striatum, and cortex but not cerebellum, MPEP inhibits DHPG-stimulated PI hydrolysis with IC50 of 8.0 nM, 20.5 nM, and 17.9 nM, respectively. MPEP positively modulates the hmGluR4 in a recombinant expression system, and the effect of MPEP is fully dependent on the activation of the orthosteric agonist L-AP4.

    In VivoWhen microiontophoretically applied into the brain of rats, MPEP reduces DHPG-induced excitations but not the excitations induced by AMPA. Following intravenous administration, MPEP produces a dose-dependent inhibition of DHPG-induced but not AMPA-induced excitations with a rapid onset of action. Oral administration of MPEP also exhibits excellent anti-hyperalgesic activity in the Complete Freund's Adjuvant and turpentine models of inflammatory pain. MPEP (1-30 mg/kg) induces anxiolytic-like effects in the conflict drinking test and the elevated plus-maze test in rats as well as in the four-plate test in mice. MPEP (1-20 mg/kg) shortens the immobility time in a tail suspension test in mice, but it is inactive in the behavioural despair test in rats. MPEP has no effect on locomotor activity or motor coordination. MPEP significantly reduces fmr1 but not wild-type center square entries and duration. In open field tests, MPEP reduces fmr1tm1Cgr center field behavior to one indistinguishable from wild-type. MPEP produces a significant reduction of total locomotor activity in three of four groups tested, at both 10 mg/kg and 30 mg/kg. 
    Animal modelMale Wistar rats, male Albino Swiss mice, or male C57BL/6J mice subjected to various tests 
    Formulation & DosageSuspended in a 1% aqueous solution of Tween 80; 30 mg/kg; i.p. or p.o. administration 
    ReferencesNeuropharmacology. 1999 Oct;38(10):1493-503; Br J Pharmacol. 2001 Apr;132(7):1423-30.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    MPEP

    Effects of MPEP and diazepam in the four-plate test in mice. Br J Pharmacol. 2001 Apr;132(7):1423-30. Br J Pharmacol. 2001 Apr;132(7):1423-30.

    MPEP

    The effects of MPEP and imipramine on the total duration of immobility in the tail suspension test in mice. Br J Pharmacol. 2001 Apr;132(7):1423-30. Br J Pharmacol. 2001 Apr;132(7):1423-30.
     


    MPEP

    The effects of MPEP and imipramine on the total duration of immobility in the forced swimming test in rats. Br J Pharmacol. 2001 Apr;132(7):1423-30.

    MPEP

    Induction of c-Fos and Hsp70 expression in cortical areas associated with psychosis after treatment with MK-801 and MPEP in adult rodents.  2012 Apr;62(5-6):2034-9.

     

    MPEP

    Dose-dependent c-Fos induction by MPEP in stress-related brain regions.  2012 Apr;62(5-6):2034-9.

     

    MPEP

    Comparison of the apoptosis induced by MPEP vs. MK-801 in the retrosplenial cortex at P7. Compared to vehicle (A) and MPEP (100 mg/kg), MK-801 (0,5 mg/kg) induces a widespread apoptosis in the cortex, including the retrosplenial cortex (C), also visible in panel D.  2012 Apr;62(5-6):2034-9.


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