Toggle Nav

MPEP Hydrochloride

Catalog No.
A3633
MGlu5 receptor antagonist
Grouped product items
SizePriceStock Qty
10mg
$60.00
Ship with 10-15 days
50mg
$230.00
Ship with 10-15 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

IC50: 36 nM

MPEP is a potent, selective and systemically active mGlu5 receptor antagonist.

Metabotropic glutamate (mGlu) receptors are a of G-protein-coupled receptor family linked to multiple second messengers and modulation of ion channel functions in the nervous system. Group I receptors (mGlu1 and -5) couple to phospholipase C and up or down regulate neuronal excitability (Gereau and Conn, 1995) whereas group II (mGlu2 and -3) and group III (mGlu4, -6, -7, and -8) receptors inhibit adenylyl cyclase and reduce synaptic transmission.

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].

Clinical trial: N/A

Reference:
[1] Gasparini F,Lingenhhl K,Stoehr N,Flor PJ,Heinrich M,Vranesic I,Biollaz M,Allgeier H,Heckendorn R,Urwyler S,Varney MA,Johnson EC,Hess SD,Rao SP,Sacaan AI,Santori EM,Velielebi G,Kuhn R.  2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist. Neuropharmacology.1999 Oct;38(10):1493-503.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt229.7
Cas No.219911-35-0
FormulaC14H12ClN
SolubilitySoluble in DMSO
Chemical Name2-methyl-6-(2-phenylethynyl)pyridine;hydrochloride
SDFDownload SDF
Canonical SMILESCC1=CC=CC(=N1)C#CC2=CC=CC=C2.Cl
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37°C and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

MPEP Hydrochloride