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MPEP
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MPEP图片
CAS NO:96206-92-7
包装与价格:
包装价格(元)
50mg电议
100mg电议
250mg电议
500mg电议
1 g电议

产品介绍
MPEP 是有效的、选择性的、非竞争性的、口服有效的、具有系统活性的mGlu5受体拮抗剂,其完全抑制quisqualate 刺激的磷酸肌醇水解的IC50值为 36 nM。MPEP 具有抗焦虑或抗抑郁活性。
生物活性

MPEP is a potent, selective, noncompetitive, orally active and systemically activemGlu5 receptorantagonist, with anIC50of 36 nM for completely inhibiting quisqualate-stimulated phosphoinositide (PI) hydrolysis. MPEP has anxiolytic-or antidepressant-like effects[1][2].

IC50& Target[1]

mGluR5

36 nM (IC50)

体外研究
(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[1].

体内研究
(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[2].
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[2].
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)[2].
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[2].

Animal Model:Male Wistar rats (200 ± 250 g)[2].
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)[2].
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).
分子量

193.24

性状

Solid

Formula

C14H11N

CAS 号

96206-92-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month