ChemicalBook > CAS DataBase List > MPEP HYDROCHLORIDE

MPEP HYDROCHLORIDE

Product Name
MPEP HYDROCHLORIDE
CAS No.
219911-35-0
Chemical Name
MPEP HYDROCHLORIDE
Synonyms
NSC1876;NSC-1876;NSC 1876;MPEP Hydrochloride, >98%;MPEP hydrochloride, 10 mM in DMSO;6-methyl-2-(phenylethynyl)pyridine;MPEP hydrochloride (DMSO Solution);MPEP hydrochloride, mGlu5 antagonist;Pyridine, 6-methyl-2-(phenylethynyl)-;2-methyl-6-(phenylethynyl)pyridine(MPEP)
CBNumber
CB0498261
Molecular Formula
C14H11N.ClH
Formula Weight
229.709
MOL File
219911-35-0.mol
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MPEP HYDROCHLORIDE Property

Melting point:
145-146℃
storage temp. 
room temp
solubility 
DMSO: 10 mg/mL
form 
solid
color 
off-white
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.
InChIKey
PKDHDJBNEKXCBI-UHFFFAOYSA-N
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Safety

WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H226Flammable liquid and vapour

H320Causes eye irritation

H336May cause drowsiness or dizziness

Precautionary statements

P210Keep away from heat/sparks/open flames/hot surfaces. — No smoking.

P233Keep container tightly closed.

P240Ground/bond container and receiving equipment.

P241Use explosion-proof electrical/ventilating/lighting/…/equipment.

P242Use only non-sparking tools.

P243Take precautionary measures against static discharge.

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P303+P361+P353IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P337+P313IF eye irritation persists: Get medical advice/attention.

P370+P378In case of fire: Use … for extinction.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P403+P235Store in a well-ventilated place. Keep cool.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
M5435
Product name
6-Methyl-2-(phenylethynyl)pyridine hydrochloride
Purity
≥98% (HPLC)
Packaging
5mg
Price
$118
Updated
2025/07/31
Sigma-Aldrich
Product number
M5435
Product name
6-Methyl-2-(phenylethynyl)pyridine hydrochloride
Purity
≥98% (HPLC)
Packaging
25mg
Price
$398
Updated
2025/07/31
Cayman Chemical
Product number
14536
Product name
MPEP (hydrochloride)
Purity
≥98%
Packaging
5mg
Price
$49
Updated
2024/03/01
Cayman Chemical
Product number
14536
Product name
MPEP (hydrochloride)
Purity
≥98%
Packaging
10mg
Price
$82
Updated
2024/03/01
Cayman Chemical
Product number
14536
Product name
MPEP (hydrochloride)
Purity
≥98%
Packaging
25mg
Price
$190
Updated
2024/03/01
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MPEP HYDROCHLORIDE Chemical Properties,Usage,Production

Description

Glutamate, the major excitatory neurotransmitter in the brain, acts on both ionotropic and metabotropic glutamate receptors. Excessive metabotropic glutamate receptor (mGluR) transmission has been linked to epilepsy, ischemia, pain, anxiety, and depression. Eight subtypes (1-8) and multiple splice variants of the mGluR have been identified and grouped based on their pharmacological properties. Group I mGluRs (subtypes 1 and 5) activate the phosphatidyl inositol pathway, while Group II (2 and 3) and Group III (4, 6, 7 and 8) inhibit adenylyl cyclase. MPEP is a potent, highly selective non-competitive antagonist at the mGlu5a receptor subtype (IC50 = 36 nM) while having no agonist or antagonist activities at the mGlu1b receptor at concentrations up to 30 μM. MPEP is centrally active following systemic administration in vivo, inducing anxiolytic-like effects in rodent models of anxiety and depression when administered at 1-30 mg/kg. MPEP has also been reported as a positive allosteric modulator of mGluR4 at μM concentrations.

Uses

Glutamate, the major excitatory neurotransmitter in the brain, acts on both ionotropic and metabotropic glutamate receptors. Excessive metabotropic glutamate receptor (mGluR) transmission has been linked to epilepsy, ischemia, pain, anxiety, and depression. Eight subtypes (1-8) and multiple splice variants of the mGluR have been identified and grouped based on their pharmacological properties. Group I mGluRs (subtypes 1 and 5) activate the phosphatidyl inositol pathway, while Group II (2 and 3) and Group III (4, 6, 7 and 8) inhibit adenylyl cyclase. MPEP is a potent, highly selective non-competitive antagonist at the mGlu5a receptor subtype (IC50 = 36 nM) while having no agonist or antagonist activities at the mGlu1b receptor at concentrations up to 30 μM. MPEP is centrally active following systemic administration in vivo, inducing anxiolytic-like effects in rodent models of anxiety and depression when administered at 1-30 mg/kg. MPEP has also been reported as a positive allosteric modulator of mGluR4 at μM concentrations.

Uses

MPEP is a potent and highly selective non-competitive mGlu5a receptor antagonist (1,2). It is also a positive allosteric modulator at mGlu4 receptors.MPEP exhibits anxiolytic and antidepressant properties that may be applicable for treating schizophrenia (3).

Definition

ChEBI: 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 positive allosteric modulator at mGlu4 receptors. Centrally active following systemic administration in vivo. Reverses mechanical hyperalgesia in the inflamed rat hind paw.

General Description

GRIN2B (glutamate ionotropic receptor NMDA type subunit 2B) codes for N-methyl d-aspartate receptor subtype 2B (GluN2B). It belongs to the N-methyl-D-aspartate receptor (NMDAR) gene family. It is located on chromosome 12p13.1.

Biochem/physiol Actions

GRIN2B (glutamate ionotropic receptor NMDA type subunit 2B) plays an important role in the growth of neurons and is highly essential for learning and memory. GRIN2B mutation is associated with neuropsychiatric and developmental disorders like schizophrenia, Parkinson′s disease and bipolar disorder. MPEP (2-methyl-6-(phenylethynyl)pyridine?hydrochloride) is used to treat Alzheimer′s disease (AD).

in vitro

in recombinant expressed cells human mglu5a receptor, mpep inhibited quisqualate-stimulated phosphoinositide hydrolysis completely with an ic50 value of 36 nm whereas with no agonist or antagonist activities at cells expressing the human mglu1b receptor. mpep did not show agonist or antagonist activity on human mglu2, -3, -4a, -7b, and -8a receptors [1].

in vivo

in rat neonatal brain slices, mpep inhibited dhpg-stimulated phosphoinositide hydrolysis with a potency and selectivity similar to that observed on human mglu receptors. moreover, in extracellular recordings in the hippocampus ca1 area of anesthetized rats, the microiontophoretic application of dhpg induced neuronal firing that was blocked when mpep was administered [1].

IC 50

36 nm

storage

+4°C (desiccate)

References

[1] FABRIZIO GASPARINI . 2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist[J]. Neuropharmacology, 1999, 38 10: Pages 1493-1503. DOI:10.1016/s0028-3908(99)00082-9
[2] JESPER MOSOLFF MATHIESEN. Positive allosteric modulation of the human metabotropic glutamate receptor 4 (hmGluR4) by SIB-1893 and MPEP[J]. British Journal of Pharmacology, 2009, 138 6: 1026-1030. DOI:10.1038/sj.bjp.0705159
[3] NICOLAS MORIN . Effect of the metabotropic glutamate receptor type 5 antagonists MPEP and MTEP in parkinsonian monkeys[J]. Neuropharmacology, 2010, 58 7: Pages 981-986. DOI:10.1016/j.neuropharm.2009.12.024
[4] NICOLAS MORIN . MPEP, an mGlu5 receptor antagonist, reduces the development of l-DOPA-induced motor complications in de novo parkinsonian monkeys: Biochemical correlates[J]. Neuropharmacology, 2013, 66: Pages 355-364. DOI:10.1016/j.neuropharm.2012.07.036
[5] AUBIN MICHALON. Chronic pharmacological mGlu5 inhibition corrects fragile X in adult mice.[J]. Neuron, 2012, 74 1: 49-56. DOI:10.1016/j.neuron.2012.03.009
[6] YOAN MIHOV G H. Negative Allosteric Modulators of Metabotropic Glutamate Receptors Subtype 5 in Addiction: a Therapeutic Window.[J]. International Journal of Neuropsychopharmacology, 2016, 19 1. DOI:10.1093/ijnp/pyw002

MPEP HYDROCHLORIDE Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from MPEP HYDROCHLORIDE manufacturers

Career Henan Chemical Co
Product
MPEP HYDROCHLORIDE 219911-35-0
Price
US $1.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
200kg
Release date
2020-01-02
Hebei Jimi Trading Co., Ltd.
Product
MPEP hydrochloride/219911-35-0/99% purity with low price in stock 219911-35-0
Price
US $1.00/kg
Min. Order
1 KG
Purity
99%
Supply Ability
20tons
Release date
2019-03-26

219911-35-0, MPEP HYDROCHLORIDERelated Search:


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