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| | Ro 25-6981 (Maleate) Basic information |
| Product Name: | Ro 25-6981 (Maleate) | | Synonyms: | [R-(R*,S*)]-α-(4-Hydroxyphenyl)-β-methyl-4-(phenylmethyl)-1-piperidinepropanol maleate salt;1-Piperidinepropanol, α-(4-hydroxyphenyl)-β-methyl-4-(phenylmethyl)-, ( αR,βS)-, (2Z)-2-butenedioate (1:1);Ro 25-6981 maleate salt, NR2B antagonist;Ro 25-6981 maleate salt (mM/ml), NR2B antagonist | | CAS: | 1312991-76-6 | | MF: | C26H33NO6 | | MW: | 455.55 | | EINECS: | | | Product Categories: | API | | Mol File: | 1312991-76-6.mol |  |
| | Ro 25-6981 (Maleate) Chemical Properties |
| storage temp. | 2-8°C | | solubility | H2O: soluble2mg/mL (clear solution, warmed) | | form | powder | | color | white to beige | | Optical Rotation | [α]/D +15 to +22°, c = 1 in methanol | | Water Solubility | H2O: 2mg/mL (clear solution, warmed) | | InChIKey | FYJZEHCQSUBZDY-SEELMCCHSA-N | | SMILES | OC(=O)\C=C/C(O)=O.C[C@@H](CN1CCC(CC1)Cc2ccccc2)[C@@H](O)c3ccc(O)cc3 |
| Hazard Codes | Xi,N | | Risk Statements | 36/37/38-50 | | Safety Statements | 26-61 | | RIDADR | UN 3077 9 / PGIII | | WGK Germany | 3 | | Storage Class | 11 - Combustible Solids |
| | Ro 25-6981 (Maleate) Usage And Synthesis |
| Uses | Ro 25-6981 maleate is a potent NMDA receptor antagonist. | | Definition | 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+). | | Biochem/physiol Actions | 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. | | in vivo | 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. |
| | IC 50 | NMDA Receptor | | storage | Room temperature (desiccate) |
| | Ro 25-6981 (Maleate) Preparation Products And Raw materials |
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