Ro 25-6981 Maleate

Research use only, not for human use.

Ro 25-6981 Maleate is a potent and selective activity-dependent NMDA receptor blocker, specifically targeting the NR2B subunit (IC50 values are 0.009 μM for NR1C/NR2B and 52 μM for NR1C/NR2A receptor subunit combinations).

Ro 25-6981 Maleate is a potent, selective and activity-dependent NR2B subunit specific NMDA receptor antagonist. Ro 25-6981 Maleat shows anticonvulsant and anti-parkinsonian activity. Ro 25-6981 Maleate has the potential for the research of parkinson's disease (PD).

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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.Ro 25-6981 Maleate (1,3 mg/kg; i.p.) exhibits age- and activation-dependent anticonvulsant action at early postnatal development in rats.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. Animal Model:6-OHDA-lesioned rats 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 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.

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Membrane Transporter/Ion Channel

NMDAR

NMDAR

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1312991-76-6

455.54

C26H33NO6

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (219.52 mM; Ultrasonic ) H2O : 8.33 mg/mL (18.29 mM; ultrasonic and warming and heat to 45°C)

OC(=O)\C=C/C(O)=O.C[C@@H](CN1CCC(Cc2ccccc2)CC1)[C@@H](O)c1ccc(O)cc1

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(-20℃)

With Ice Pack

≥ 2 years