MPEP

Catalog No.S2809 Batch:S280901

Print

Technical Data

Formula

C14H11N
Molecular Weight 193.24 CAS No. 96206-92-7
Solubility (25°C)* In vitro DMSO 39 mg/mL (201.82 mM)
Ethanol 39 mg/mL (201.82 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description MPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM, and this compound exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors.
Targets
mGluR5 [1]
36 nM
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, this compound 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, it inhibits DHPG-stimulated PI hydrolysis with IC50 of 8.0 nM, 20.5 nM, and 17.9 nM, respectively. [1] This chemical positively modulates the hmGluR4 in a recombinant expression system, and the effect is fully dependent on the activation of the orthosteric agonist L-AP4. [3]
In vivo When microiontophoretically applied into the brain of rats, MPEP reduces DHPG-induced excitations but not the excitations induced by AMPA. Following intravenous administration, this compound produces a dose-dependent inhibition of DHPG-induced but not AMPA-induced excitations with a rapid onset of action. Oral administration of this chemical also exhibits excellent anti-hyperalgesic activity in the Complete Freund's Adjuvant and turpentine models of inflammatory pain. [1] It (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. This compound (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. It has no effect on locomotor activity or motor coordination. [2] This chemical significantly reduces fmr1 but not wild-type center square entries and duration. In open field tests, it reduces fmr1tm1Cgr center field behavior to one indistinguishable from wild-type. It produces a significant reduction of total locomotor activity in three of four groups tested, at both 10 mg/kg and 30 mg/kg. [4]
Features Inactive against other group I/II/III metabotropic glutamate receptors.

Protocol (from reference)

Animal Study:[2]
  • Animal Models

    Male Wistar rats, male Albino Swiss mice, or male C57BL/6J mice subjected to various tests

  • Dosages

    ~30 mg/kg

  • Administration

    Administered intraperitoneally (i.p.) or perorally (p.o.) at 60 minutes before the tests

References

  • https://pubmed.ncbi.nlm.nih.gov/10530811/
  • https://pubmed.ncbi.nlm.nih.gov/11264235/
  • https://pubmed.ncbi.nlm.nih.gov/12684257/
  • https://pubmed.ncbi.nlm.nih.gov/16054174/

Customer Product Validation

The expression of mGluR5 and Homer were detected by Western blot and analysed by ImageJ. a–c Cells were treated with various concentrations of pu-erh tea for 12 h. d–f Cells were treated with 62.5 μg/mL pu-erh tea for 3, 6, 9, 12 h. g-i Cells were treated with 62.5 μg/mL pu-erh, black, or green teas for 12 h. Data were analysed using GraphPad Prism software (***p < 0.001 vs. vehicle control, **p < 0.01 vs. vehicle control, n = 3)

Data from [ , , Mol Neurobiol, 2017, 54(7):5286-5299 ]

Selleck's MPEP Has Been Cited by 1 Publication

Pu-erh Tea Protects the Nervous System by Inhibiting the Expression of Metabotropic Glutamate Receptor 5. [Li C, et al. Mol Neurobiol, 2017, 54(7):5286-5299] PubMed: 27578019

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.