| Identification | Back Directory | [Name]
Ro 25-6981 (Maleate) | [CAS]
1312991-76-6 | [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) | [Molecular Formula]
C26H33NO6 | [MDL Number]
MFCD06798375 | [MOL File]
1312991-76-6.mol | [Molecular Weight]
455.543 |
| Chemical Properties | Back Directory | [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) |
| Hazard Information | Back Directory | [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]
Store at -20°C |
|
| Company Name: |
Sigma-Aldrich
|
| Tel: |
021-61415566 800-8193336 |
| Website: |
https://www.sigmaaldrich.cn |
| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
|