Ro 25-6981

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Ro 25-6981 是一种有效的选择性活性依赖性 NMDA 受体阻滞剂，含有 NR2B 亚基，对于克隆受体亚基组合 NR1C/NR2B 和 NR1C/NR2A 的 IC50 值分别为 0.009 和 52 μM。 Ro 25-6981 可用于帕金森病的研究。

Ro 25-6981 is a potent and selective activity-dependent NMDA receptors blocker containing the NR2B subunit with IC50s of 0.009 and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A respectively. Ro 25-6981 can be used in studies about Parkinson's disease.(In Vivo):Ro 25-6981 (800 μg; intrathecally) shows significant analgesic effects on incision pain in rats and effectively attenuates postoperative hyperalgesia induced by remifentanil. In 6-OHDA-lesioned rats, Ro 25-6981 (0.39-12.5 mg/kg; i.p.) dose-dependently induces contraversive rotations without stimulating locomotion in normal rats. In male albino rats of Wistar strain, Ro 25-6981 (1 and 3 mg/kg; i.p.) exhibits activation- and age-dependent anticonvulsant action at early postnatal development and causes a significant decrease of N1–P2 amplitude at higher stimulation intensities at 3 mg/kg.

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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.Ro 25-6981 (1,3 mg/kg; i.p.) exhibits age- and activation-dependent anticonvulsant action at early postnatal development in rats.Ro 25-6981 (800 μg; intrathecal injection) shows significant analgesic effects on incision pain in rats and effectively attenuated postoperative hyperalgesia. 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 strainDosage: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

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169274-78-6

339.479

C22H29NO2

>98% (HPLC)

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C[C@@H](CN1CCC(Cc2ccccc2)CC1)[C@@H](O)c1ccc(O)cc1

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(-20℃)

With Ice Pack

≥ 2 years