| Identification | Back Directory | [Name]
(AR,BS)-ALPHA-(4-HYDROXYPHENYL)-BETA-METHYL-4-(PHENYLMETHYL)-1-PIPERIDINEPROPANOL MALEATE | [CAS]
169274-78-6 | [Synonyms]
CS-2705
RO 25-6981 MALEATE
Ro 25-6981 maleate salt
(αR,βS)-α-(4-Hydroxyphenyl)-β-methyl-4-(phenylmethyl)-1-piperidinepropanol
1-Piperidinepropanol, α-(4-hydroxyphenyl)-β-methyl-4-(phenylmethyl)-, (αR,βS)-
(αR,βS)-α-(4-Hydroxyphenyl)-β-methyl-4-(phenylmethyl)-1-piperidinepropanolmaleate
(aR,bS)-a-(4-Hydroxyphenyl)-b-methyl-4-(phenylmethyl)-1-piperidinepropanol maleate
(alphaR,betaS)-alpha-(4-Hydroxyphenyl)-beta-methyl-4-(phenylmethyl)-1-piperidinepropanol
(AR,BS)-ALPHA-(4-HYDROXYPHENYL)-BETA-METHYL-4-(PHENYLMETHYL)-1-PIPERIDINEPROPANOL MALEATE
(alpha-R,beta-S)-alpha-(4-Hydroxyphenyl)-beta-methyl-4-(phenylmethyl)-1-piperidinepropanolmaleate | [Molecular Formula]
C22H29NO2 | [MDL Number]
MFCD06798375 | [MOL File]
169274-78-6.mol | [Molecular Weight]
339.47 |
| Chemical Properties | Back Directory | [Boiling point ]
512.4±45.0 °C(Predicted) | [density ]
1.116±0.06 g/cm3(Predicted) | [storage temp. ]
Desiccate at RT | [solubility ]
DMSO : 100 mg/mL (294.58 mM; Need ultrasonic) | [form ]
Powder | [pka]
10.01±0.26(Predicted) | [color ]
White to off-white | [Water Solubility ]
H2O: 25mM |
| Hazard Information | Back Directory | [Uses]
Ro 25-6981 maleate is a potent NMDA receptor antagonist. | [Definition]
ChEBI: Ro 25-6981 is a member of the class of piperidines that is 4-benzylpiperidine substituted by a 3-hydroxy-3-(4-hydroxyphenyl)-2-methylpropyl group at position 1 (the 1R,2S-stereoisomer). It is a potent antagonist of the GluN2B subunit of the N-methyl-D-aspartate (NMDA) receptor. It has a role as a NMDA receptor antagonist, an anticonvulsant, an antidepressant and a neuroprotective agent. It is a member of piperidines, a member of phenols, a secondary alcohol, a tertiary amino compound and a member of benzenes. It is a conjugate base of a Ro 25-6981(1+). | [Biological Activity]
Potent and selective activity-dependent blocker of NMDA receptors containing the NR2B subunit. IC 50 values are 0.009 and 52 μ M for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A respectively. Displays neuroprotectant effects in vivo and in vitro . | [in vivo]
Ro 25-6981 (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 (1,3 mg/kg; i.p.) exhibits age- and activation-dependent anticonvulsant action at early postnatal development in rats[2].
Ro 25-6981 (800 μg; intrathecal injection) shows significant analgesic effects on incision pain in rats and effectively attenuated postoperative hyperalgesia[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 |
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