| Description | Gavestinel sodium is a noncompetitive NMDA receptor antagonist with potency, selectivity, and oral activity.Gavestinel sodium binds to the glycine site of the NMDA receptor with a binding affinity (pKi value) of 8.5.Gavestinel sodium is used in acute ischemic stroke studies. |
| In vivo | Gavestinel sodium（800 mg）作为起始剂量给药后，维持剂量分别为100 mg、200 mg或400 mg，每12小时给药一次，连续五次。Gavestinel sodium 的平均末端半衰期介于29小时至56小时之间。Gavestinel sodium 在血浆中的结合率极高（中位数游离百分比<0.01）。在Gavestinel sodium 给药期间，部分患者出现胆红素水平升高，这可能与排除机制（糖醛酸结合和胆汁排泄）的共享有关。[2] |
| Target activity | NMDAR:8.5(pKi) |
| Synonyms | GV 150526, Gavestinel sodium salt |
| molecular weight | 397.19 |
| Molecular formula | C18H11Cl2N2NaO3 |
| CAS | 153436-38-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 90.0 mg/mL (226.6 mM), Sonication is recommended. |
| References | 1. Di Fabio R, et al. Substituted indole-2-carboxylates as in vivo potent antagonists acting as the strychnine-insensitive glycine binding site. J Med Chem. 1997;40(6):841-850. 2. Hoke JF, et al. Pharmacokinetics of a glycine site antagonist (gavestinel) following multiple dosing in patients with acute stroke. Eur J Clin Pharmacol. 2000;55(11-12):867-872. 3. Lees KR, et al. Glycine antagonist (gavestinel) in neuroprotection (GAIN International) in patients with acute stroke: a randomised controlled trial. GAIN International Investigators. Lancet. 2000;355(9219):1949-1954. 4. Haley EC Jr, et al. Gavestinel does not improve outcome after acute intracerebral hemorrhage: an analysis from the GAIN International and GAIN Americas studies. Stroke. 2005;36(5):1006-1010. |