MPEP 96206-92-7

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Molecular Weight: 193.24 MPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM, exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors.

Biological Activity

MPEP has no appreciable agonist or antagonist activity at the closely
related recombinant human mGlu1b receptor expressed in CHO-K1 cells or a
purinoreceptor endogenously expressed in L(tk-) cells up to
concentrations of 100 μM. Furthermore, MPEP shows no appreciable agonist
or antagonist activity in cAMP accumulation or [35S]-GTPγS
binding assays at the recombinant human group II and III metabotropic
receptors (human mGlu2, -3, -4a, -6, -7b, -8a) as well as the human NMDA
(NMDAR1A/2A, -1A/2B), rat AMPA (GluR3) and human kainate (GluR6)
receptor subtypes. In slices of rat neonatal hippocampus, striatum, and
cortex but not cerebellum, MPEP inhibits DHPG-stimulated PI hydrolysis
with IC50 of 8.0 nM, 20.5 nM, and 17.9 nM, respectively. MPEP positively modulates the hmGluR4 in a recombinant expression
system, and the effect of MPEP is fully dependent on the activation of
the orthosteric agonist L-AP4.






When
microiontophoretically applied into the brain of rats, MPEP reduces
DHPG-induced excitations but not the excitations induced by AMPA.
Following intravenous administration, MPEP produces a dose-dependent
inhibition of DHPG-induced but not AMPA-induced excitations with a rapid
onset of action. Oral administration of MPEP also exhibits excellent
anti-hyperalgesic activity in the Complete Freund's Adjuvant and
turpentine models of inflammatory pain. MPEP (1-30 mg/kg)
induces anxiolytic-like effects in the conflict drinking test and the
elevated plus-maze test in rats as well as in the four-plate test in
mice. MPEP (1-20 mg/kg) shortens the immobility time in a tail
suspension test in mice, but it is inactive in the behavioural despair
test in rats. MPEP has no effect on locomotor activity or motor
coordination. MPEP significantly reduces fmr1 but not wild-type center square entries and duration. In open field tests, MPEP reduces fmr1tm1Cgr center field behavior to one indistinguishable from wild-type. MPEP
produces a significant reduction of total locomotor activity in three of
four groups tested, at both 10 mg/kg and 30 mg/kg.

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Product Categories : Neuronal Signaling > GluR Inhibitor