MPEP hydrochloride is an effective and highly specific non-competitive antagonist at the mGlu5 receptor subtype (IC50: 36 nM).
Images & Validation
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Key Properties
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CAS Number
219911-35-0
MW
229.7
Purity
>98% (HPLC)
Formula
C14H12ClN
SMILES
c1(ccccc1)C#Cc1cccc(n1)C.Cl
Target
mGluR
Solubility
H2O : ≥ 50 mg/mL; 217.68 mM
Bioactivity
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In Vivo
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) does shorten the immobility time in a tail suspension test in mice, however it is inactive in the behavioural despair test in rats. MPEP (30 mg/kg i.p.) slightly but significantly increases (by 39%) the number of punished crossings in the four-plate test, lower doses of the compound (3 and 10 mg/kg) does not affect the number of punished crossings in that test (F (3, 36) = 3.240, P<0.05). MPEP (1, 10 and 20 mg/kg) significantly (by 55% after the highest dose), (F(3, 28) = 15.47, P<0.001) decreases the immobility time of mice in the tail suspension test. Its efficacy is similar to that of imipramine (20 mg/kg), used as the positive standard. Animal model: Male Wistar rats (200 ± 250 g). Dosage: IP or PO. Administration: 0.3, 1 and 10 mg/kg, i.p. (Conflict drinking test). Result: At a dose of 0.3 mg/kg was not ffective, at doses of 1 and 10 mg/kg i.p. significantly (F (3, 30) = 11.193, P<0.001), increased the number of shocks (by 330 and 507%, respectively) accepted during the experimental session in the Vogel test. Animal model: Male Wistar rats (200 ± 250 g). Dosage: IP or PO. Administration: 1, 3 and 10 mg/kg, i.p. or 10 and 30 mg/kg, p.o. (Elevated plus-maze test). Result: Administered at a dose of 1 mg kg71 i.p. did not change the entries into and time spent in the open arms. At doses of 3 and 10 mg/kg i.p. significantly (F (3, 24) = 22.978, P<0.001) dose-dependently increased the time spent in the open arms (up to 45 and 74%, respectively), and the percentage of entries into the open arms (up to 48 and 68%, respectively, F(3, 24) = 5.678, P<. 01). At doses of 3 and 10 mg/kg i.p. significantly increased (by 64%) the total number of entries and reduced (by about 25%) the total time. spent (data not shown) in the arms (either type). At the dose of 30 mg/kg (po, but not 10 mg/kg) significantly (up to 64%, F (2, 16) = 14.249, P<0.001) increased the percentage of the time spent in the open arms and the percentage of entries into the open arms (up to 63%, F (2, 16) = 7.295, P<0.01). MPEP given p.o. in both doses used did not change the total number of entries nor the total time spent in the arms (either type).
In Vitro
MPEP does not show agonist or antagonist activity at 100 mM on human mGlu2, -3, -4a, -7b, and -8a receptors nor at 10 μM on the human mGlu6 receptor.
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