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L-701324

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Chemical Structure| 142326-59-8 同义名 : -
CAS号 : 142326-59-8
货号 : A560344
分子式 : C21H14ClNO3
纯度 : 99%+
分子量 : 363.794
MDL号 : MFCD00910917
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
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：
生物活性
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].
实验方案
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
参考文献

[1]Bristow LJ, Flatman KL, et al. The atypical neuroleptic profile of the glycine/N-methyl-D-aspartate receptor antagonist, L-701,324, in rodents. J Pharmacol Exp Ther. 1996 May;277(2):578-85.

[2]Bristow LJ, Hutson PH, et al. Anticonvulsant and behavioral profile of L-701,324, a potent, orally active antagonist at the glycine modulatory site on the N-methyl-D-aspartate receptor complex. J Pharmacol Exp Ther. 1996 Nov;279(2):492-501.

[3]Wlaź P, Poleszak E. Differential effects of glycine on the anticonvulsant activity of D-cycloserine and L-701,324 in mice. Pharmacol Rep. 2011;63(5):1231-4

[4]Bristow LJ, Hutson PH, Kulagowski JJ, Leeson PD, Matheson S, Murray F, Rathbone D, Saywell KL, Thorn L, Watt AP, Tricklebank MD. Anticonvulsant and behavioral profile of L-701,324, a potent, orally active antagonist at the glycine modulatory site on the N-methyl-D-aspartate receptor complex. J Pharmacol Exp Ther. 1996 Nov;279(2):492-501

[5]Konieczny J, Ossowska K, Schulze G, Coper H, Wolfarth S. L-701,324, a selective antagonist at the glycine site of the NMDA receptor, counteracts haloperidol-induced muscle rigidity in rats. Psychopharmacology (Berl). 1999 Apr;143(3):235-43

[6]Bristow LJ, Flatman KL, Hutson PH, Kulagowski JJ, Leeson PD, Young L, Tricklebank MD. The atypical neuroleptic profile of the glycine/N-methyl-D-aspartate receptor antagonist, L-701,324, in rodents. J Pharmacol Exp Ther. 1996 May;277(2):578-85

[7]Obrenovitch TP, Hardy AM, Zilkha E. Effects of L-701,324, a high-affinity antagonist at the N-methyl-D-aspartate (NMDA) receptor glycine site, on the rat electroencephalogram. Naunyn Schmiedebergs Arch Pharmacol. 1997 Jun;355(6):779-86