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编 号:F454424
分子式:C20H19NO4
分子量:337.37
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10mM*1mL in DMSO
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5mg
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10mg
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50mg
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生物活性:
Dizocilpine maleate (MK-801 maleate) is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes.

体内研究:
Dizocilpine maleate 可用于动物建模,构建精神分裂模型。Dizocilpine maleate (0.2 mg/kg,腹腔注射) 在 SD 大鼠体内的半衰期为 52.31 分钟,AUC 为 3185.48 nM·min,清除率为 34 nM。诱导精神分裂模型致病原理Dizocilpine maleate 诱导精神分裂的具体机制尚不清楚。一种假设是 Dizocilpine maleate 通过抑制 NMDA 致使谷氨酸能系统失调,从而诱导精神分裂。 具体造模方法Rats: Sprague-Dawley • male • adult with weigh of 250-300 gAdministration: 0.4 mg/kg • 腹腔注射. • 单剂量Note造模成功指标行为:自发活动增加并伴有明显的焦虑样行为,具体表现为较远距离运动活动增加 (多动),在中心区停留时间减少 (回避中心区)。前脉冲抑制 (PPI):PPI 显著降低。迷宫测试:在高架十字迷宫测试中表现为避免进入开阔臂,在 Y 迷宫测试中表现为减少进入新臂同类产品: Phencyclidine拮抗产品:Clozapine (HY-14539); Haloperidol (HY-14538)

体外研究:
[3H]Dizocilpine maleate binds with NMDA receptor with a Kd of 37.2±2.7 nM in rat cerebral cortical membranes.Dizocilpine maleate causes a progressive, long-lasting blockade of current induced by N-Me-D-Asp.Dizocilpine maleate progressively suppresses of current induced by NMDA. Mg2+ (10 mM) prevents Dizocilpine from blocking the N-Me-D-Asp-induced current, even when Dizocilpine (MK-801) is applied for a long time in the presence of NMDA. Dizocilpine blocks NMDA-activated single-channel activity in outside-out patches. Dizocilpine maleate (Dizocilpine maleate 相关抗体:
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