化合物MPEP T6598
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
5 mg | 96206-92-7 | ¥247.00 | 询底价 |
10 mg | 96206-92-7 | ¥413.00 | 询底价 |
25 mg | 96206-92-7 | ¥787.00 | 询底价 |
500 mg | 96206-92-7 | ¥5,330.00 | 询底价 |
200 mg | 96206-92-7 | ¥3,330.00 | 询底价 |
50 mg | 96206-92-7 | ¥1,380.00 | 询底价 |
1 mg | 96206-92-7 | ¥119.00 | 询底价 |
1 mL | 96206-92-7 | ¥253.00 | 询底价 |
2 mg | 96206-92-7 | ¥159.00 | 询底价 |
100 mg | 96206-92-7 | ¥2,230.00 | 询底价 |
Product Introduction
Bioactivity
英文名: MPEP
描述: MPEP 是一种选择性 mGlu5 受体拮抗剂,IC50 为 36 nM,有抗焦虑和抗抑郁活性。
体外活性: MPEP has no appreciable agonist or antagonist activity at the closely related recombinant human mGlu1b receptor expressed in CHO-K1 cells or a purinoreceptor endogenously expressed in L(tk-) cells up to concentrations of 100 μM. Furthermore, MPEP shows no appreciable agonist or antagonist activity in cAMP accumulation or [35S]-GTPγS binding assays at the recombinant human group II and III metabotropic receptors (human mGlu2, -3, -4a, -6, -7b, -8a) as well as the human NMDA (NMDAR1A/2A, -1A/2B), rat AMPA (GluR3) and human kainate (GluR6) receptor subtypes. In slices of rat neonatal hippocampus, striatum, and cortex but not cerebellum, MPEP inhibits DHPG-stimulated PI hydrolysis with IC50 of 8.0 nM, 20.5 nM, and 17.9 nM, respectively. [1] MPEP positively modulates the hmGluR4 in a recombinant expression system, and the effect of MPEP is fully dependent on the activation of the orthosteric agonist L-AP4. [3]
体内活性: When microiontophoretically applied into the brain of rats, MPEP reduces DHPG-induced excitations but not the excitations induced by AMPA. Following intravenous administration, MPEP produces a dose-dependent inhibition of DHPG-induced but not AMPA-induced excitations with a rapid onset of action. Oral administration of MPEP also exhibits excellent anti-hyperalgesic activity in the Complete Freund's Adjuvant and turpentine models of inflammatory pain. [1] 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) shortens the immobility time in a tail suspension test in mice, but it is inactive in the behavioural despair test in rats. MPEP has no effect on locomotor activity or motor coordination. [2] MPEP significantly reduces fmr1 but not wild-type center square entries and duration. In open field tests, MPEP reduces fmr1tm1Cgr center field behavior to one indistinguishable from wild-type. MPEP produces a significant reduction of total locomotor activity in three of four groups tested, at both 10 mg/kg and 30 mg/kg. [4]
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 37 mg/mL (191.5 mM)
Ethanol : 37 mg/mL (191.5 mM)
关键字: Metabotropic glutamate receptors | inhibit | mGluR | Inhibitor | MPEP
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