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  3. MPEP Hydrochloride

MPEP Hydrochloride 

Cat. No.: HY-14609 Purity: 99.69%
Handling Instructions

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

For research use only. We do not sell to patients.

MPEP Hydrochloride Chemical Structure

MPEP Hydrochloride Chemical Structure

CAS No. : 219911-35-0

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Description

MPEP hydrochloride is a potent and highly selective non-competitive antagonist at the mGlu5 receptor subtype with IC50 of 36 nM. IC50 Value: 36 nM Target: mGluR in vitro: 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. in vivo: 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.

Molecular Weight

229.70

Formula

C₁₄H₁₂ClN

CAS No.

219911-35-0

SMILES

CC1=NC(C#CC2=CC=CC=C2)=CC=C1.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : ≥ 50 mg/mL (217.68 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.3535 mL 21.7675 mL 43.5350 mL
5 mM 0.8707 mL 4.3535 mL 8.7070 mL
10 mM 0.4354 mL 2.1768 mL 4.3535 mL
*Please refer to the solubility information to select the appropriate solvent.
References

Purity: 99.69%

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Keywords:

MPEPmGluRMetabotropic glutamate receptorsInhibitorinhibitorinhibit

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MPEP Hydrochloride
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