货号	规格	价格	上海	北京	珠海	重庆	武汉
S88678-5mg买3赠1	≥98%	￥135.00 S88678-5mg ￥135.00 2-3天（买3赠1）	0 货期：2-3天	-	-	-	-
S88678-10mg买3赠1	≥98%	￥260.00 S88678-10mg ￥260.00 2-3天（买3赠1）	0 货期：2-3天	-	-	-	-
S88678-25mg	≥98%	￥600.00 S88678-25mg ￥600.00 2-3天	0 货期：2-3天	-	-	-	-
S88678-100mg	≥98%	￥1830.00 S88678-100mg ￥1830.00 2-3天	0 货期：2-3天	-	-	-	-

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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

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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