Ro 25-6981 maleate is a potent NMDA receptor antagonist.
ChEBI: Ro 25-6981 maleate is the maleic acid salt of Ro 25-6981. It is a potent and selective antagonist of GluN2B-containing NMDA receptors. It has a role as an anticonvulsant, an antidepressant, a neuroprotective agent and a NMDA receptor antagonist. It contains a Ro 25-6981(1+).
Ro 25-6981 maleate salt is a potent and selective antagonist of NMDA glutamate receptors containing the NR2B subunit with IC50 values of .009 μM for NR2B vs. 52 μM for NR2A subunits. Ro 25-6981 has been shown to have neuroprotectant effects and to reduce inflammatory and neuropathic pain in rodent models.
Ro 25-6981 Maleate (0.39-12.5 mg/kg; i.p.) induces contraversive rotations in 6-hydroxydopamine (6-OHDA)-lesioned rats without stimulating locomotion in normal rats[1].
Ro 25-6981 Maleate (1,3 mg/kg; i.p.) exhibits age- and activation-dependent anticonvulsant action at early postnatal development in rats[2].
Ro 25-6981 Maleate (800 μg; intrathecal injection) shows significant analgesic effects on incision pain in rats and effectively attenuated postoperative hyperalgesia induced by remifentanil[3].
| Animal Model: | 6-OHDA-lesioned rats[1] |
| Dosage: | 0.39-12.5 mg/kg |
| Administration: | I.p. |
| Result: | Dose-dependently induced contraversive tight nose-to-tail rotations, and induced a weak ipsiversive circling response indicating a mild unspecific stimulatory action of the compound. |
| Animal Model: | Male albino rats of Wistar strain[2] |
| Dosage: | 1, 3 mg/kg |
| Administration: | I.p. |
| Result: | Caused a significant decrease of N1–P2 amplitude at higher stimulation intensities AT 3 mg/kg, and exhibited age- and activation-dependent anticonvulsant action at early postnatal development. |
Room temperature (desiccate)
