Name | MPEP HYDROCHLORIDE |
Synonyms | MPEP HYDROCHLORIDE 6-methyl-2-(phenylethynyl)pyridine Pyridine, 6-methyl-2-(phenylethynyl)- 2-methyl-6-(phenylethynyl)pyridine(MPEP) MPVP replace pvp,White Crystal, New Stock! 6-Methyl-2-(phenylethynyl)pyridine hydrochloride |
CAS | 219911-35-0 |
InChIKey | PKDHDJBNEKXCBI-UHFFFAOYSA-N |
Molecular Formula | C14H11N.ClH |
Molar Mass | 229.709 |
Melting Point | 145-146℃ |
Solubility | DMSO: 10mg/mL |
Appearance | solid |
Color | off-white |
Storage Condition | room temp |
Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month. |
In vitro study | 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. |
In vivo study | 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 and mg i.p. significantly increased the total number entries reduced about time spent not shown in arms 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). |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 4.353 ml | 21.767 ml | 43.533 ml |
5 mM | 0.871 ml | 4.353 ml | 8.707 ml |
10 mM | 0.435 ml | 2.177 ml | 4.353 ml |
5 mM | 0.087 ml | 0.435 ml | 0.871 ml |
biological activity | MPEP Hydrochloride is potent, selective, non-competitive, orally effective, A systemically active mGlu5 receptor antagonist has an IC50 value of 36 nM for the complete inhibition of the hydrolysis of phosphoinositide stimulated by quisqualate. MPEP Hydrochloride has anti-Anxiety or antidepressant activity. |
Target | mGluR5 36 nM (IC 50 ) |
in vitro study | MPEP does not show Agar or antagonist activity at 100 mM on human mGlu2, -3, -4a, -7b, and -8a receptors nor at 10 μm on the human mGlu6 receptor. |
in vivo study | MPEP (1-30mg/kg) induced anxiolytic-like effects in the conflict beverage 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 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 and mg I .p. significantly increased the total number entries reduced about time spent not shown in arms 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). |
Animal Model: | Male Wistar rats (200 ± 250 g). Male Wistar rats (200 ± 250 g). |
Dosage: | IP or PO. IP or PO. |
Administration: | 0.3, 1 and 10 mg/kg, i.p. (Conflict drinking test). 1, 3 and 10 mg/kg, i.p. or 10 and 30 mg/kg, p.o.(Elevated plus-maze 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. 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 and mg i.p. significantly increased the total number entries reduced about time spent not shown in arms 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). |