• 产品描述： Radiprodil (RGH-896) is an orally active and selective NMDA NR2B receptors antagonist. It was a potential treatment of neuropathic pain associated with diabetic peripheral neuropathy (DPNP)

• 靶点： NMDAR; iGluR;NMDAR; iGluR

• 体外研究：
  The inhibition potency of ligands toward the NR2B NMDA receptors was evaluated by measuring the Ca2þ influx evocated by NMDA application (at 100 mM for 30 s) in NR1a/NR2B subunit transfected HEK cells. Radiprodil had potent inhibitory effects (69 nM) towards Ca2+ influx . A low concentration (10 nM) of the GLUN2B receptor antagonist Radiprodil restored LTP in the presence of Aβ1-42, 3NTyr10-Aβ, Aβ1-40, but not AβpE3. Radiprodil (10 nM) reversed the synaptic toxicity of Aβ species but not that of AβpE3 .

• 体内研究：
  The in vivo analgesic efficiency for 1a in the mouse formalin test was 7.7 mg/kg p.o. (ED50) and a clinical trial is currently conducted with Radiprodil .

• 动物实验： Chronically treated Sprague–Dawley rats were administered fluoxetine (18 mg/kg/day) or SNAP 94847 (20 mg/kg/day) via oral gavage in 20% beta-cyclodextrin for 2 weeks (1 injection, 6 h into light cycle). For acute treatment, drugs were given orally in 20% betacyclodextrin 1 h before testing. On each test day, locomotor activity was recorded during a 60 min habituation to the novel locomotor cage, after which the rats were administered quinpirole (0.3 mg/kg, i.p.) and returned immediately to the cage, where locomotor activity was measured for an additional 180 min. In each case-control animals were administered the corresponding vehicle, without drug

• 参考文献：
  1. Labas R, et al. Synthesis, evaluation and metabolic studies of radiotracers containing a 4-(4-[18F]-fluorobenzyl)piperidin-1-yl moiety for the PET imaging of NR2B NMDA receptors. Eur J Med Chem. 2011 Jun;46(6):2295-309.
  2. Rammes G, et al. The NMDA receptor antagonist Radiprodil reverses the synaptotoxic effects of different amyloid-beta (Aβ) species on long-term potentiation (LTP). Neuropharmacology. 2018 Sep 15;140:184-192.
  3. Mullier B, et al. GRIN2B gain of function mutations are sensitive to radiprodil, a negative allosteric modulator of GluN2B-containing NMDA receptors. Neuropharmacology. 2017 Sep 1;123:322-331.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20°C

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.516 ml	12.582 ml	25.164 ml
  5 mM	0.503 ml	2.516 ml	5.033 ml
  10 mM	0.252 ml	1.258 ml	2.516 ml
  50 mM	0.05 ml	0.252 ml	0.503 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *