MPEP (Hydrochloride)

Names

[ CAS No. ]:
219911-35-0

[ Name ]:
MPEP (Hydrochloride)

[Synonym ]:
6-Methyl-2-(phenylethynyl)pyridine hydrochloride
2-Methyl-6-(phenylethynyl)pyridine hydrochloride
Pyridine,6-methyl-2-(phenylethynyl)
MPEP (Hydrochloride)
Pyridine, 2-methyl-6-(2-phenylethynyl)-, hydrochloride (1:1)
2-Methyl-6-(phenylethynyl)pyridine hydrochloride (1:1)
6-methyl-2-(phenylethynyl)pyridine
MPEP HYDROCHLORIDE

Biological Activity

[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 nMTarget: mGluRin 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.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> mGluR

Research Areas >> Neurological Disease

[References]

[1]. Inta, Dragos; Filipovic, Dragana; Lima-Ojeda, Juan M. et al. The mGlu5 receptor antagonist MPEP activates specific stress-related brain regions and lacks neurotoxic effects of the NMDA receptor antagonist MK-801: Significance for the use as anxiolytic/ant

[2]. Chau, Peipei; Soederpalm, Bo; Ericson, Mia The mGluR5 antagonist MPEP elevates accumbal dopamine and glycine levels; interaction with strychnine-sensitive glycine receptors. Addiction Biology (2011), 16(4), 591-599.

[3]. D'Souza, Manoranjan S.; Markou, Athina Metabotropic glutamate receptor 5 antagonist 2-methyl-6-(phenylethynyl)pyridine (MPEP) microinfusions into the nucleus accumbens shell or ventral tegmental area attenuate the reinforcing effects of nicotine in rats.

[Related Small Molecules]

mavoglurant | L-Glutamine | CTEP (RO4956371) | LY 354740 | L-(+)Sodium glutamate | ADX-88178 | FITM | (S)-MCPG | Basimglurant | LY341495 | Dipraglurant | JNJ-40411813 | LY404039 | JNJ 16259685 | ADX-47273

Chemical & Physical Properties

[ Density]:
1.1g/cm3

[ Boiling Point ]:
336.3ºC at 760mmHg

[ Molecular Formula ]:
C₁₄H₁₂ClN

[ Molecular Weight ]:
229.705

[ Flash Point ]:
144.8ºC

[ Exact Mass ]:
229.065826

[ PSA ]:
12.89000

[ LogP ]:
3.59180

[ Appearance of Characters ]:
light yellow solid

[ Vapour Pressure ]:
0.000221mmHg at 25°C

[ Index of Refraction ]:
1.614

[ Storage condition ]:
-20℃

MSDS

Click to get detail MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3

[ HS Code ]:
2933399090

Customs

[ HS Code ]: 2933399090

[ Summary ]:
2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Articles

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Emerging evidence indicates that type I metabotropic glutamate receptors (mGluRs) in the nucleus accumbens play a critical role in cocaine seeking. The present study sought to determine the role of ac...

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