MPEP Hydrochloride is a potent, selective, noncompetitive, orally active mGlu5 receptor antagonist with an IC50 of 36 nM for inhibiting quisqualate-stimulated phosphoinositide hydrolysis. It exhibits anxiolytic and antidepressant-like effects[1][2]. MPEP Hydrochloride serves as a click chemistry reagent, containing an Alkyne group that can participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) with Azide-containing molecules.
体内研究
MPEP (1-30 mg/kg) elicits anxiolytic-like effects in various behavioral tests, including the conflict drinking test and the elevated plus-maze test in rats, as well as the four-plate test in mice[2].
MPEP (1-20 mg/kg) reduces the immobility time in a tail suspension test in mice, though it shows no activity in the behavioral despair test in rats[2].
MPEP (30 mg/kg i.p.) significantly increases the number of punished crossings by 39% in the four-plate test, whereas lower doses (3 and 10 mg/kg) do not affect punished crossings in that test (F (3,36)=3.240, P<0.05)[2].
MPEP administered at 1, 10, and 20 mg/kg significantly reduces the immobility time in the tail suspension test in mice by up to 55% after the highest dose (F(3,28)=15.47, P<0.001), demonstrating efficacy comparable to that of imipramine (20 mg/kg), which is used as the positive control[2].
体外研究
MPEP does not exhibit agonistic or antagonistic effects at 100 mM on human mGlu2, -3, -4a, -7b, and -8a receptors, nor at 10 μM on the human mGlu6 receptor[1].
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