MPEP Hydrochloride

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MPEP Hydrochloride

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。

CAS NO:

219911-35-0

包装与价格：

包装	价格(元)
10 mM * 1 mL in Water	电议
10mg	电议
50mg	电议
100mg	电议
200mg	电议

产品介绍

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。

生物活性

MPEP Hydrochloride is a potent, selective, noncompetitive, orally active and systemically activemGlu5 receptorantagonist, with anIC₅₀of 36 nM for completely inhibiting quisqualate-stimulated phosphoinositide (PI) hydrolysis. MPEP Hydrochloride 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

229.70

性状

Solid

Formula

C₁₄H₁₂ClN

CAS 号

219911-35-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

H₂O : 25 mg/mL(108.84 mM;ultrasonic and warming and heat to 80℃)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	4.3535 mL	21.7675 mL	43.5350 mL
5 mM	0.8707 mL	4.3535 mL	8.7070 mL
10 mM	0.4354 mL	2.1768 mL	4.3535 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.
请依序添加每种溶剂： Saline
Solubility: 100 mg/mL (435.35 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。