MW 229.7 Da, Purity >99%. Subtype selective and potent non-competitive mGlu5 antagonist (IC50 = 36 nM). Central effects following systemic administration in vivo.
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GLUR, GPRC1E, GRM5_HUMAN, Glutamate receptor metabotropic 5, Metabotropic glutamate receptor 5, Metabotropic glutamate receptor 5 variant F, Metabotropic glutamate receptor 5 variant G, Metabotropic glutamate receptor 5 variant H, PPP1R86, Protein phosphatase 1 regulatory subunit 86, Smp_128940, mGlu5, mGluR5
MW 229.7 Da, Purity >99%. Subtype selective and potent non-competitive mGlu5 antagonist (IC50 = 36 nM). Central effects following systemic administration in vivo.
Soluble in water to 5 mM, in ethanol to 100 mM and in DMSO to 100 mM.
Subtype selective and potent non-competitive mGlu5 antagonist (IC50 = 36 nM). Central effects following systemic administration in vivo.
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2D chemical structure image of ab120008, MPEP hydrochloride, mGlu5 antagonist
Basal PLD activity is strongly stimulated by the D1/5R agonist and blocked by the D1/5R, mGluR5, mGluR1, and the PLD-linked mGluR antagonists in the amygdala of cocaine CPP animals.
The dotted line indicates PLD activity associated with control slices (no EtOH added) which was determined for each animal and used to calculate the change in PLD activity levels with EtOH and/or drug application.
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 (PPADS, P2 purinergic receptor antagonist ab120009) (n=9), and MPEP+PPADS (n=3). A single asterisk (*) indicates p<0.05; double asterisks (**), p<0.01.
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 (PPADS, P2 purinergic receptor antagonist 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.
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