L-701324 is an orally active and long acting anticonvulsant with high affinity and selectivity for the glycine site on the NMDA receptor.
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产品名称 | NMDA receptor ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Empirical Formula | ✔ | 97% | |||||||||||||||||
Dizocilpine maleate |
+++
NMDA receptor, Kd: 37.2 nM | 99%+ | |||||||||||||||||
Felbamate |
+
NMDAR, IC50: 1.8 mM | 98% | |||||||||||||||||
(-)-Dizocilpine maleate |
++++
NMDA receptor, Ki: 30.5 nM | 98% | |||||||||||||||||
Ifenprodil tartrate |
+++
NMDA Receptor, IC50: 0.3 μM | 98% | |||||||||||||||||
Spermidine | ✔ | Autophagy | 98% GC | ||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | L-701324 is an orally active and long acting anticonvulsant with high affinity and selectivity for the glycine site on the NMDA receptor. L-701,324 produced a marked increase in the seizure threshold, which was significantly reversed by the administration of glycine[3]. In contrast to N-methyl-D-aspartate receptor ion channel blockers such as MK-801 (dizocilpine), L-701,324 is a potent, p.o. active anticonvulsant with a reduced propensity to activate mesolimbic dopaminergic systems in rodents[4]. L-701324 (2.5-40 mg/kg, i.p.) dose-dependently decreased the muscle tone enhanced by haloperidol (1-5 mg/kg, i.p.). L-701324 exhibits a beneficial action in the animal model of parkinsonian rigidity, but not that of parkinsonian akinesia[5]. Pretreatment with L-701,324 dose-dependently antagonized amphetamine-induced hyperactivity in the mouse (ED50 = 1.12 +/- 0.45 mg/kg p.o.), an effect which was similar to that of the classical neuroleptic, haloperidol, and the atypical neuroleptic, clozapine. In addition, p.o. administration of L-701,324 (2.5 or 5 mg/kg) attenuated the hyperactivity response induced by amphetamine infusion into the rat nucleus accumbens. L-701,324 failed to impair spontaneous locomotor activity or induce catalepsy in the mouse at doses > or = 100 mg/kg[6]. Moreover, anticonvulsant and neuroprotective actions of L-701,324 may not be associated with marked anaesthesia-like side-effects[7]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM | 2.75mL 0.55mL 0.27mL | 13.74mL 2.75mL 1.37mL | 27.49mL 5.50mL 2.75mL |
CAS号 | 142326-59-8 |
分子式 | C21H14ClNO3 |
分子量 | 363.794 |
别名 | |
运输 | 蓝冰 |
存储条件 | 液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Room Temperature |
溶解度 | DMSO: 35 mg/mL(96.21 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |