| 名称 | PEAQX tetrasodium hydrate |
| 描述 | PEAQX tetrasodium hydrate (PEAQX tetrasodium hydrate (459836-30-7 free base)) is an orally available NMDA antagonist that is potent and selective. The IC50 value of PEAQX tetrasodium hydrate (459836-30-7 free base) against hNMDAR 1A/2A was 270 nM and 29600 nM against hNMDAR 1A/2B, respectively. |
| 体外活性 | PEAQX has a high binding affinity for NMDA receptors (IC50=8 nM), and a functional preference in excess of 100-fold for hNMDA 1A/2A (IC50=of 270 nM) over 1A/2B receptors (IC50=29,600 nM).[1] |
| 体内活性 | PEAQX is practically inactive in Xenopus oocytes expressing hNMDA 1A/2B receptors, displays an ED50 value of 23 mg/kg in the MES test [1].
Sprague-Dawley rats were treated on PN7, PN9, and PN11 with PCP (10 mg/kg), PEAQX (NR2A-preferring antagonist; 10, 20, or 40 mg/kg), or ifenprodil (selective NR2B antagonist; 1, 5, or 10 mg/kg) and sacrificed for measurement of caspase-3 activity (an index of apoptosis) or allowed to age and tested for locomotor sensitization to PCP challenge on PN28-PN35. PCP or PEAQX on PN7, PN9, and PN11 markedly elevated caspase-3 activity in the cortex; ifenprodil showed no effect. Striatal apoptosis was evident only after subchronic treatment with a high dose of PEAQX (20 mg/kg). Animals treated with PCP or PEAQX on PN7, PN9, and PN11 showed a sensitized locomotor response to the PCP challenge on PN28-PN35.[2] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | H2O : 22.9 mg/mL (41.0 mM), Sonication and heating are recommended.
|
| 关键字 | 459836-30-7 free base | 459836-30-7 | NVP-AAM077 tetrasodium Hydrate | PEAQX tetrasodium Hydrate |
| 相关产品 | Stavudine | 5-Fluorouracil | Acetylcysteine | Kaempferol | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Metronidazole | Sorafenib | Tributyrin | Lidocaine hydrochloride |
| 相关库 | 疼痛相关化合物库 | 神经退行性疾病化合物库 | 经典已知活性库 | 神经信号分子库 | 膜蛋白靶向化合物库 | 已知活性化合物库 |
United States
