Subtype selective and potent non-competitive mGlu5 antagonist (IC50 = 36 nM). Central effects following systemic administration in vivo.
Store at +4°C. Store under desiccating conditions. The product can be stored for up to 12 months.
Soluble in water to 5 mM, in ethanol to 100 mM and in DMSO to 100 mM
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Functional Studies - MPEP hydrochloride (ab120008)Image from Gómez-Gonzalo M et al., PLoS Biol. 2010;8(4):e1000352. Fig 2.; doi: 10.1371/journal.pbio.1000352.
Astrocyte Ca2+ signal inhibition does not affect interictal discharges. (A–D) Mean percentage of astrocytes activated by the ictal discharges (A), mean duration (B) and frequency (C) of the ictal discharge, and mean frequency of interictal discharges (D) under different experimental conditions in EC slice preparations. Controls (n=16), MPEP (ab120008) (n=7), PPADS (ab120009) (n=9), and MPEP+PPADS (n=3). A single asterisk (*) indicates p<0.05; double asterisks (**), p<0.01.
Functional Studies - MPEP hydrochloride (ab120008)Image from Gómez-Gonzalo M et al., PLoS Biol. 2010;8(4):e1000352. Fig 6(A).; doi: 10.1371/journal.pbio.1000352.
Ca2+ signal from a field A neuron, a field B neuron, and field A astrocytes in response to repetitive episodes of NMDA stimulation (black arrowheads). The NMDA stimulation that evoked an ictal discharge became ineffective after blocking the astrocyte response by bath perfusion with MPEP (ab120008) and PPADS (ab120009). An ictal discharge could be recovered by increasing the number of NMDA puffs (white arrowheads). A double NMDA pulse evoked both astrocyte activation and the ictal discharge after inhibitor washout.
MPEP hydrochloride (ab120008)参考文献
This product has been referenced in:
Malherbe P et al. Mutational analysis and molecular modeling of the binding pocket of the metabotropic glutamate 5 receptor negative modulator 2-methyl-6-(phenylethynyl)-pyridine. Mol Pharmacol64:823-32 (2003).
Read more (PubMed: 14500738) »
Salt TE et al. Antagonism of the mGlu5 agonist 2-chloro-5-hydroxyphenylglycine by the novel selective mGlu5 antagonist 6-methyl-2-(phenylethynyl)-pyridine (MPEP) in the thalamus. Br J Pharmacol127:1057-9 (1999).
Read more (PubMed: 10455248) »
Gasparini F et al. 2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist. Neuropharmacology38:1493-503 (1999).
Read more (PubMed: 10530811) »