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MPEP Hydrochloride

Catalog No.GC16172

A potent, highly selective mGlu5a receptor antagonist

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MPEP Hydrochloride Chemical Structure

Cas No.: 219911-35-0

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10mg
$45.00
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50mg
$181.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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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

Cas No. 219911-35-0 SDF
Chemical Name 2-methyl-6-(2-phenylethynyl)pyridine;hydrochloride
Canonical SMILES CC1=CC=CC(=N1)C#CC2=CC=CC=C2.Cl
Formula C14H12ClN M.Wt 229.7
Solubility DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml,PBS (pH 7.2): 5 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 4.3535 mL 21.7675 mL 43.535 mL
5 mM 0.8707 mL 4.3535 mL 8.707 mL
10 mM 0.4354 mL 2.1768 mL 4.3535 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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