CAS 219911-35-0|MPEP (Hydrochloride)

Introduction：Basic information about CAS 219911-35-0|MPEP (Hydrochloride), including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. MPEP (Hydrochloride) BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Customs
6. Articles19
7. Synonyms

Common Name	MPEP (Hydrochloride)
CAS Number	219911-35-0	Molecular Weight	229.705
Density	1.1g/cm3	Boiling Point	336.3ºC at 760mmHg
Molecular Formula	C₁₄H₁₂ClN	Melting Point	/
MSDS	ChineseUSA	Flash Point	144.8ºC

Names

Name	2-methyl-6-(phenylethynyl)pyridine
Synonym	More Synonyms

MPEP (Hydrochloride) BiologicalActivity

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 >>mGluRResearch 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.

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 >>mGluRResearch 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.

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
InChIKey	PKDHDJBNEKXCBI-UHFFFAOYSA-N
SMILES	Cc1cccc(C#Cc2ccccc2)n1.Cl
Storage condition	-20℃

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%

Articles19

Group I metabotropic glutamate receptor-mediated activation of PKC gamma in the nucleus accumbens core promotes the reinstatement of cocaine seeking.

Addict. Biol. 20(2) , 285-96, (2015)

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...

Endocannabinoids mediate bidirectional striatal spike-timing-dependent plasticity.

J. Physiol. 593 , 2833-49, (2015)

Although learning can arise from few or even a single trial, synaptic plasticity is commonly assessed under prolonged activation. Here, we explored the existence of rapid responsiveness of synaptic pl...

Estradiol mediates dendritic spine plasticity in the nucleus accumbens core through activation of mGluR5.

Brain Struct. Funct. 220 , 2415-22, (2015)

Accumulating evidence from human and rodent studies suggests that females are more sensitive to the motivating and rewarding properties of drugs of abuse. Numerous reports implicate estradiol in enhan...

Synonyms

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

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