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Purity: ≥98%
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.
| ln Vitro |
At 100 mM on human mGlu2, -3, -4a, -7b, and -8a receptors, as well as at 10 μM on the human mGlu6 receptor, MPEP exhibits neither agonist nor antagonist activity[1].
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| ln Vivo |
In the conflict drinking test, the elevated plus-maze test, and the four-plate test in mice, MPEP (1-30 mg/kg) causes anxiolytic-like effects[2]. In a tail suspension test, MPEP (1–20 mg/kg) does reduce the immobility period in mice; however, in a behavioral despair test, it had no effect in rats[2]. Lower doses of the chemical (3 and 10 mg/kg) have no effect on the number of punished crossings in the four-plate test (F (3,36)=3.240, P<0.05)[2]. However, MPEP (30 mg/kg ip) marginally but significantly increases (by 39%) the number of punished crossings in that test. Mice immobility time in the tail suspension test is considerably reduced by MPEP (1, 10 and 20 mg/kg) (F(3,28)=15.47, P<0.001), with a 55% reduction observed after the highest dose. Its effectiveness is comparable to the positive standard imipramine (20 mg/kg)[2].
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| Animal Protocol |
Animal/Disease Models: Male Wistar rats (200 ± 250 g)[2].
Doses: IP or PO. Route of Administration: 0.3, 1 and 10 mg/kg, ip (Conflict drinking test). Experimental Results: At a dose of 0.3 mg/kg was not effective, at doses of 1 and 10 mg/kg ip Dramatically (F (3,30)=11.193, P< 0.001), increased the number of shocks (by 330 and 507%, respectively) accepted during the experimental session in the Vogel test. Animal/Disease Models: Male Wistar rats (200 ± 250 g)[2]. Doses: IP or PO. Route of Administration: 1, 3 and 10 mg/kg, ip or 10 and 30 mg/kg, po(Elevated plus-maze test). Experimental Results: Administered at a dose of 1 mg kg71 ip did not change the entries into and time spent in the open arms. At doses of 3 and 10 mg/kg ip Dramatically (F (3,24)=22.978, P<0.001) dose-dependently increased the time spent in the open arms (up to 45 and 74%, respectively), and the percentage of entries into the open arms (up to 48 and 68%, respectively, F(3,24)=5.678, P<.01). At doses of 3 and 10 mg/kg ip Dramatically increased (by 64% ) the total number of en |
| References |
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| Additional Infomation |
2-methyl-6-(phenylethynyl)pyridine is a methylpyridine that coinsists of 2-methylp[yridine bearing an additional phenylethynyl group at position 6. Potent and highly selective non-competitive antagonist at the mGlu5 receptor subtype (IC50 = 36 nM) and a positive allosteric modulator at mGlu4 receptors. Centrally active following systemic administration in vivo. Reverses mechanical hyperalgesia in the inflamed rat hind paw. It has a role as a metabotropic glutamate receptor antagonist and an anxiolytic drug. It is a member of methylpyridines and an acetylenic compound. It is a conjugate base of a 2-methyl-6-(phenylethynyl)pyridinium(1+). It derives from a hydride of an acetylene.
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| Molecular Formula |
C14H11N
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| Molecular Weight |
193.24
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| Exact Mass |
193.089
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| CAS # |
96206-92-7
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| Related CAS # |
MPEP Hydrochloride;219911-35-0
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| PubChem CID |
3025961
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| Appearance |
Yellow to brown solid powder
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| Boiling Point |
336.3ºC at 760mmHg
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| Flash Point |
144.8ºC
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| LogP |
3.591
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
15
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| Complexity |
251
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NEWKHUASLBMWRE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H11N/c1-12-6-5-9-14(15-12)11-10-13-7-3-2-4-8-13/h2-9H,1H3
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| Chemical Name |
2-methyl-6-(2-phenylethynyl)pyridine
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (12.94 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (12.94 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 2% DMSO+30% PEG 300+5% Tween 80: 10 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.1749 mL | 25.8746 mL | 51.7491 mL | |
| 5 mM | 1.0350 mL | 5.1749 mL | 10.3498 mL | |
| 10 mM | 0.5175 mL | 2.5875 mL | 5.1749 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03506945 | Completed | Behavioral: mPEP Behavioral: Bibliotherapy |
Depressive Symptoms Stress, Psychological |
University of California, San Diego | November 1, 2018 | Not Applicable |
| NCT04439097 | Unknown † | Other: Multicomponent physical exercise program associated with a Mediterranean diet Other: Usual care |
Alzheimer Disease Physical Exercise Bone Density Fall |
University of Salamanca | September 15, 2021 | Not Applicable |
| NCT01024491 | Completed | Drug: paroxetine Drug: placebo |
Premature Ejaculation | MorePharma Corporation | August 2008 | Phase 3 |
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