MPEP hydrochloride

SKU: orb1222508

Description

MPEP hydrochloride is an effective and highly specific non-competitive antagonist at the mGlu5 receptor subtype (IC50: 36 nM).

Key Properties

• 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

• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

mGluR