2-甲基-6-(苯基乙炔基)吡啶盐酸盐
- CAS号:219911-35-0
- 英文名:MPEP HYDROCHLORIDE
- 中文名:2-甲基-6-(苯基乙炔基)吡啶盐酸盐
- CBNumber:CB0498261
- 分子式:C14H11N.ClH
- 分子量:229.709
- MOL File:219911-35-0.mol
- 熔点 :145-146℃
- 储存条件 :room temp
- 溶解度 :DMSO: 10 mg/mL
- 形态 :solid
- 颜色 :off-white
- 稳定性 :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.
- InChIKey :PKDHDJBNEKXCBI-UHFFFAOYSA-N
- WGK Germany :3
2-甲基-6-(苯基乙炔基)吡啶盐酸盐性质、用途与生产工艺
- 生物活性 MPEP Hydrochloride 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 Hydrochloride 具有抗焦虑或抗抑郁活性。
-
靶点
mGluR5
36 nM (IC 50 )
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体外研究
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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体内研究
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).
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