同义名 :	AWD 131-138; ELB138
	CAS号 :	188116-07-6
	货号 :	A202497
	分子式 :	C13H14ClN3O2
	纯度 :	99%+
	分子量 :	279.72
	MDL号 :	MFCD18450225
	存储条件：	Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

AWD 131-138 [1-(4-chlorophenyl)-4-morpholino-imidazolin-2-one], a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models. At the dose of 100 microg/kg i.v. AWD 131-138, sufficient drug was self-administered to squirrel monkeys during the first session (about 3.5 mg/kg) to produce plasma levels above 1000 ng/ml, yet responding over the next two sessions dropped to vehicle levels. The failure of AWD 131-138 to produce benzodiazepine-like discriminative effects and the absence of drug self-administration behavior when substituted for cocaine suggest that its abuse liability is low[3]. AWD 131-138 dose-dependently stimulated GABA currents. At 10 microM AWD 131-138, this allosteric stimulation amounted in average to about 12-21% of the maximal stimulation achieved using diazepam. The threshold of stimulation was about 0.3-1.0 microM[4]. Prolonged oral administration with twice-daily dosing of ELB 138 (AWD 131-138) with either 5 or 40 mg/kg over a 5-week period was not associated with loss of anticonvulsant efficacy in the PTZ (pentylenetetrazole) dog model[5].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	3.58mL 0.72mL 0.36mL	17.88mL 3.58mL 1.79mL	35.75mL 7.15mL 3.58mL

参考文献

[1]Yasar S, Bergman J, et al. Evaluation of the novel antiepileptic drug, AWD 131-138, for benzodiazepine-like discriminative stimulus and reinforcing effects in squirrel monkeys. Eur J Pharmacol. 2003 Apr 4;465(3):257-65. [2]Sigel E, Baur R, et al. The antiepileptic drug AWD 131-138 stimulates different recombinant isoforms of the rat GABA(A) receptor through the benzodiazepine binding site. Neurosci Lett. 1998 Apr 3;245(2):85-8. [3]Yasar S, Bergman J, Munzar P, Redhi G, Tober C, Knebel N, Zschiesche M, Paronis C. Evaluation of the novel antiepileptic drug, AWD 131-138, for benzodiazepine-like discriminative stimulus and reinforcing effects in squirrel monkeys. Eur J Pharmacol. 2003 Apr 4;465(3):257-65 [4]Sigel E, Baur R, Netzer R, Rundfeldt C. The antiepileptic drug AWD 131-138 stimulates different recombinant isoforms of the rat GABA(A) receptor through the benzodiazepine binding site. Neurosci Lett. 1998 Apr 3;245(2):85-8 [5]Löscher W, Potschka H, Rieck S, Tipold A, Rundfeldt C. Anticonvulsant efficacy of the low-affinity partial benzodiazepine receptor agonist ELB 138 in a dog seizure model and in epileptic dogs with spontaneously recurrent seizures. Epilepsia. 2004 Oct;45(10):1228-39