| Description | Ro 25-6981 is a potent and selective activity-dependent NMDA receptors blocker containing the NR2B subunit with IC50s of 0.009 and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A respectively. Ro 25-6981 can be used in studies about Parkinson's disease. |
| In vivo | Ro 25-6981（800 µg；脊髓内）对大鼠手术切口痛具有显著的镇痛效果，并有效减轻由芬太尼引起的术后高敏感症[3]。在6-OHDA损伤的大鼠中，Ro 25-6981（0.39-12.5 mg/kg；腹腔内）剂量依赖性地诱导逆时针旋转，但不刺激正常大鼠的运动活性[4]。在Wistar品系的雄性白大鼠中，Ro 25-6981（1和3 mg/kg；腹腔内）呈现出活化和年龄依赖的抗惊厥作用，且在早期产后发育中，在3 mg/kg剂量下显著降低在高刺激强度下的N1–P2振幅[5]。 |
| molecular weight | 339.47 |
| Molecular formula | C22H29NO2 |
| CAS | 169274-78-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 90 mg/mL (265.12 mM), Sonication is recommended. |
| References | 1. Fischer G, et al. Ro 25-6981, a highly potent and selective blocker of N-methyl-D-aspartate receptors containing the NR2B subunit. Characterization in vitro. J Pharmacol Exp Ther. 1997 Dec;283(3):1285-92. 2. Lynch DR, et al. Pharmacological characterization of interactions of RO 25-6981 with the NR2B (epsilon2) subunit. Eur J Pharmacol. 2001 Mar 30;416(3):185-95. 3. Jiang M, et al. Antinociception and prevention of hyperalgesia by intrathecal administration of Ro 25-6981, a highly selective antagonist of the 2B subunit of N-methyl-D-aspartate receptor. Pharmacol Biochem Behav. 2013 Nov;112:56-63. 4. Löschmann PA, et al. Antiparkinsonian activity of Ro 25-6981, a NR2B subunit specific NMDA receptor antagonist, in animal models of Parkinson's disease. Exp Neurol. 2004 May;187(1):86-93. 5. Szczurowska E,et al. Different action of a specific NR2B/NMDA antagonist Ro 25-6981 on cortical evoked potentials and epileptic afterdischarges in immature rats. Brain Res Bull. 2015 Feb;111:1-8. |
| Citations | 1. Liu T, Shi J, Wu D, et al.THSG alleviates cerebral ischemia/reperfusion injury via the GluN2B–CaMKII–ERK1/2 pathway.Phytomedicine.2024: 155595. |