Ro 25-6981 Maleate 是一种有效的、选择性和活性依赖性的 NR2B 亚基特异性NMDA 受体拮抗剂。Ro 25-6981 Maleat 具有抗惊厥和抗帕金森病活性。Ro 25-6981 Maleate 具有研究帕金森病(PD)的潜力。
生物活性 | Ro 25-6981 Maleate is a potent, selective and activity-dependent NR2B subunit specificNMDA receptorantagonist. 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)[1][2][3]. |
体内研究 (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. |
|
分子量 | |
性状 | |
Formula | |
CAS 号 | |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: DMSO : 100 mg/mL(219.52 mM;Need ultrasonic) H2O : 8.33 mg/mL(18.29 mM;ultrasonic and warming and heat to 45℃) 配制储备液 1 mM | 2.1952 mL | 10.9760 mL | 21.9520 mL | 5 mM | 0.4390 mL | 2.1952 mL | 4.3904 mL | 10 mM | 0.2195 mL | 1.0976 mL | 2.1952 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 5 mg/mL (10.98 mM); Clear solution
此方案可获得 ≥ 5 mg/mL (10.98 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 5 mg/mL (10.98 mM); Clear solution
此方案可获得 ≥ 5 mg/mL (10.98 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 5 mg/mL (10.98 mM); Clear solution
此方案可获得 ≥ 5 mg/mL (10.98 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
|